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ChEMBL ligand: CHEMBL118 (Celebra, Celebrex, Celecoxib, DFN-15, DFN15, Elyxyb, NSC-719627, NSC-758624, Onsenal, SC-58635) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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3-phosphoinositide dependent protein kinase 1/3-phosphoinositide dependent protein kinase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2534] [GtoPdb: 1519] [UniProtKB: O15530] | ||||||||
ChEMBL | Inhibition of recombinant PDK1 using RPRAATF as substrate by scintillation counting | B | 4.32 | pIC50 | 48000 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 1629-1632 [PMID:22266037] |
ChEMBL | Inhibition of PDK1-mediated Akt activation in human PC3 cells after 2 hrs by Western blotting analysis | B | 4.32 | pIC50 | 48000 | nM | IC50 | Eur J Med Chem (2013) 65: 323-336 [PMID:23735281] |
ChEMBL | In Vitro Kinase Assay: PDK-1 kinase activity This in vitro assay was performed using a PDK-1 kinase assay kit (Upstate, Lake Placid, N.Y.) according to the vendor's instructions. This cell-free assay is based on the ability of recombinant PDK-1, in the presence of DMSO vehicle or the test agent, to activate its downstream kinase serum- and glucocorticoid-regulated kinase (SGK.) which, in turn, phosphorylates the Akt/SGK-specific peptide substrate RPRAATF with [Îł-32]-ATP. The [32P]-phosphorylated peptide substrate was then separated from the residual [Îł-32P]-ATP using PS1 phosphocellulose paper and quantitated by a scintillation counter after three washes with 0.75% phosphoric acid. | B | 4.32 | pIC50 | 48000 | nM | IC50 | US-8741944-B2. Anti-infective agents against intracellular pathogens (2014) |
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8] | ||||||||
ChEMBL | DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA) | B | 4.86 | pKi | 13917 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Adenosine A3 radioligand binding (ligand: AB-MECA) | B | 4.61 | pIC50 | 24622 | nM | IC50 | DrugMatrix in vitro pharmacology data |
AGAP002992-PA in Anopheles gambiae (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3399914] [UniProtKB: Q5TU56] | ||||||||
ChEMBL | Inhibition of Anopheles gambiae carbonic anhydrase pre-incubated for 15 mins by stopped-flow CO2 hydration assay | B | 6.76 | pKi | 173 | nM | Ki | Bioorg Med Chem (2015) 23: 2303-2309 [PMID:25882523] |
α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089] | ||||||||
ChEMBL | DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) | B | 6.16 | pKi | 692 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine) | B | 5.82 | pIC50 | 1516 | nM | IC50 | DrugMatrix in vitro pharmacology data |
Alpha carbonic anhydrase in Stylophora pistillata (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075028] [UniProtKB: B5SU02] | ||||||||
ChEMBL | Inhibition of cloned Stylophora pistillata alpha-CA expressed in human HEK293 cells by stopped-flow CO2 assay | B | 7.47 | pKi | 34.2 | nM | Ki | Bioorg Med Chem (2009) 17: 5054-5058 [PMID:19520577] |
ChEMBL | Inhibition of Stylophora pistillata carbonic anhydrase by stopped-flow CO2 hydration assay | B | 7.47 | pKi | 34.2 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 710-714 [PMID:21208801] |
15-LOX-1/Arachidonate 15-lipoxygenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2903] [GtoPdb: 1388] [UniProtKB: P16050] | ||||||||
ChEMBL | Inhibition of 15-LOX (unknown origin) | B | 7.31 | pIC50 | 49 | nM | IC50 | RSC Med Chem (2022) 13: 471-496 [PMID:35685617] |
5-LOX/Arachidonate 5-lipoxygenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL215] [GtoPdb: 1385] [UniProtKB: P09917] | ||||||||
ChEMBL | Inhibition of 5LOX in human whole blood assessed as inhibition of calcium ionophore A 23187-stimulated 5HETE production by HPLC analysis | F | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2004) 47: 6195-6206 [PMID:15566290] |
ChEMBL | Inhibition of 5-LOX (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2023) 80: 129101-129101 [PMID:36481449] |
ChEMBL | Inhibition of 5-LOX (unknown origin) using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition and measured after 10 mins | B | 5.76 | pIC50 | 1720 | nM | IC50 | Eur J Med Chem (2020) 189: 112066-112066 [PMID:31982653] |
Astrosclerin-3 in Astrosclera willeyana (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1944499] [UniProtKB: A6YCJ1] | ||||||||
ChEMBL | Inhibition of GST-tagged astrosclera willeyana Astrosclerin-3 expressed in Escherichia coli after 15 mins preincubation by stopped flow CO2 hydration assay | B | 6.14 | pKi | 732 | nM | Ki | Bioorg Med Chem (2012) 20: 1403-1410 [PMID:22285172] |
β3-adrenoceptor/Beta-3 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL246] [GtoPdb: 30] [UniProtKB: P13945] | ||||||||
ChEMBL | DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol) | B | 4.92 | pKi | 12093 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Adrenergic beta3 radioligand binding (ligand: [125I] Cyanopindolol) | B | 4.79 | pIC50 | 16124 | nM | IC50 | DrugMatrix in vitro pharmacology data |
Carbonate dehydratase in Sulfurihydrogenibium sp. (strain YO3AOP1) (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3745586] [UniProtKB: B2V8E3] | ||||||||
ChEMBL | Inhibition of recombinant Sulfurihydrogenibium yellowstonense YO3AOP1 carbonic anhydrase by stopped flow CO2 hydrase assay | B | 8.16 | pKi | 6.9 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 401-405 [PMID:26691758] |
Carbonic anhydrase in Mycobacterium tuberculosis (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6068] [UniProtKB: P9WPJ9] | ||||||||
ChEMBL | Inhibition of full length Mycobacterium tuberculosis H37Rv recombinant carbonic anhydrase 2 encoded by RV3588c by stopped flow CO2 hydration assay | B | 6.15 | pKi | 713 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 6649-6654 [PMID:19846301] |
ChEMBL | Inhibition of Mycobacterium tuberculosis recombinant carbonic anhydrase Rv3588c pre-incubated for 15 mins by stopped-flow CO2 hydration method | B | 6.15 | pKi | 713 | nM | Ki | J Med Chem (2012) 55: 9619-9629 [PMID:23067387] |
Carbonic anhydrase in Methanosarcina thermophila (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3932] [UniProtKB: P40881] | ||||||||
ChEMBL | Inhibitory activity against alpha carbonic anhydrase (Co-Cam) from Methanosarcina thermophila | B | 6 | pKi | 1010 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 6001-6006 [PMID:15546717] |
ChEMBL | Inhibitory activity against alpha carbonic anhydrase (Zn-Cam) from Methanosarcina thermophila | B | 6.85 | pKi | 140 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 6001-6006 [PMID:15546717] |
Carbonic anhydrase in Stylophora pistillata (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1649055] [UniProtKB: C0IX24] | ||||||||
ChEMBL | Inhibition of Stylophora pistillata carbonic anhydrase 2 by stopped-flow CO2 hydration assay | B | 6.16 | pKi | 690 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 710-714 [PMID:21208801] |
Carbonic anhydrase in Methanobacterium thermoautotrophicum (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3926] [UniProtKB: Q50565] | ||||||||
ChEMBL | Inhibitory activity against beta carbonic anhydrase (Cab) from Methanobacterium thermoautotrophicum | B | 4.41 | pKi | 38500 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 6001-6006 [PMID:15546717] |
Carbonic anhydrase in Candida albicans (strain SC5314 / ATCC MYA-2876) (Yeast) (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5337] [UniProtKB: Q5AJ71] | ||||||||
ChEMBL | Inhibition of Candida albicans recombinant Nce103 by stopped-flow CO2 hydration assay | B | 5.99 | pKi | 1017 | nM | Ki | Bioorg Med Chem (2009) 17: 4503-4509 [PMID:19450983] |
ChEMBL | Inhibition of Candida albicans CaNce103 preincubated for 15 mins measured for 10 to 100 sec by stopped-flow method | B | 5.99 | pKi | 1017 | nM | Ki | J Med Chem (2012) 55: 3513-3520 [PMID:22424239] |
Carbonic anhydrase in Candida glabrata CBS 138 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6185] [UniProtKB: Q6FTL6] | ||||||||
ChEMBL | Inhibition of recombinant full length Candida glabrata NCE103 expressed in Escherichia coli BL21 preincubated for 15 mins by stopped-flow CO2 hydrase assay | B | 6.94 | pKi | 116 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 2647-2652 [PMID:23511020] |
Carbonic anhydrase in Saccharomyces cerevisiae S288c (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5931] [UniProtKB: P53615] | ||||||||
ChEMBL | Inhibition of Saccharomyces cerevisiae recombinant CA expressed in Escherichia coli by stopped-flow CO2 hydrase assay | B | 6.97 | pKi | 108 | nM | Ki | Bioorg Med Chem (2009) 17: 1158-1163 [PMID:19124253] |
Carbonic anhydrase 15 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5973] [UniProtKB: Q99N23] | ||||||||
ChEMBL | Inhibition of mouse recombinant carbonic anhydrase 15 by stopped flow CO2 hydrase assay | B | 7.35 | pKi | 45 | nM | Ki | J Med Chem (2009) 52: 646-654 [PMID:19193158] |
ChEMBL | Inhibition of mouse recombinant carbonic anhydrase 15 after 15 mins by stopped-flow CO2 hydration assay | B | 7.35 | pKi | 45 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 4376-4381 [PMID:20605094] |
Carbonic anhydrase 2 in Cryptococcus neoformans var. grubii (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1697676] [UniProtKB: Q3I4V7] | ||||||||
ChEMBL | Inhibition of Cryptococcus neoformans Can2 preincubated for 15 mins measured for 10 to 100 sec by stopped-flow method | B | 5.51 | pKi | 3056 | nM | Ki | J Med Chem (2012) 55: 3513-3520 [PMID:22424239] |
Carbonic anhydrase, alpha family in Thiomicrospira crunogena (strain XCL-2) (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3621035] [UniProtKB: Q31FD6] | ||||||||
ChEMBL | Inhibition of recombinant Thiomicrospira crunogena XCL-2 carbonic anhydrase by stopped flow CO2 hydrase assay | B | 6.01 | pKi | 981 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 401-405 [PMID:26691758] |
carbonic anhydrase 1/Carbonic anhydrase I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL261] [GtoPdb: 2597] [UniProtKB: P00915] | ||||||||
ChEMBL | Inhibition of full length human cytosolic carbonic anhydrase 1 preincubated for 15 mins by stop flow CO2 hydrase assay | B | 4.3 | pKi | 50000 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 4184-4190 [PMID:27485387] |
ChEMBL | Inhibitory activity against human carbonic anhydrase I at 0.09 uM | B | 4.3 | pKi | 50000 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 6001-6006 [PMID:15546717] |
ChEMBL | Inhibitory activity against cloned human CA1 | B | 4.3 | pKi | 50000 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 437-442 [PMID:16290146] |
ChEMBL | Inhibition of human recombinant carbonic anhydrase 1 by stopped flow CO2 hydration method | B | 4.3 | pKi | 50000 | nM | Ki | J Med Chem (2009) 52: 2226-2232 [PMID:19317447] |
ChEMBL | Inhibition of human recombinant CA1 by stopped-flow CO2 hydrase assay | B | 4.3 | pKi | 50000 | nM | Ki | Bioorg Med Chem (2009) 17: 1158-1163 [PMID:19124253] |
ChEMBL | Inhibition of human recombinant carbonic anhydrase 1 by stopped flow CO2 hydrase assay | B | 4.3 | pKi | 50000 | nM | Ki | J Med Chem (2009) 52: 646-654 [PMID:19193158] |
ChEMBL | Inhibition of human recombinant carbonic anhydrase 1 by stopped flow CO2 hydration assay | B | 4.3 | pKi | 50000 | nM | Ki | J Med Chem (2009) 52: 3116-3120 [PMID:19338333] |
ChEMBL | Inhibition of human recombinant carbonic anhydrase 1 by stopped-flow CO2 hydrase method | B | 4.3 | pKi | 50000 | nM | Ki | Bioorg Med Chem (2009) 17: 4503-4509 [PMID:19450983] |
ChEMBL | Inhibition of human recombinant CA1 by stopped-flow CO2 assay | B | 4.3 | pKi | 50000 | nM | Ki | Bioorg Med Chem (2009) 17: 5054-5058 [PMID:19520577] |
ChEMBL | Inhibition of human recombinant carbonic anhydrase 1 after 15 mins by stopped-flow CO2 hydration assay | B | 4.3 | pKi | 50000 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 4376-4381 [PMID:20605094] |
ChEMBL | Inhibition of wild type human recombinant carbonic anhydrase 1 expressed in Escherichia coli BL21 (DE3) after 15 mins by CO2 hydration method | B | 4.3 | pKi | 50000 | nM | Ki | Bioorg Med Chem (2010) 18: 5498-5503 [PMID:20624682] |
ChEMBL | Inhibition of human recombinant CA1 by stopped-flow CO2 hydration assay | B | 4.3 | pKi | 50000 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 710-714 [PMID:21208801] |
ChEMBL | Inhibition of human carbonic anhydrase I by spectrophotometry at pH 7.5 | B | 4.3 | pKi | 50000 | nM | Ki | Bioorg Med Chem (2011) 19: 1172-1178 [PMID:21251841] |
ChEMBL | Inhibition of human recombinant carbonic anhydrase 1 at pH 7.5 by stopped flow CO2 hydration assay | B | 4.3 | pKi | 50000 | nM | Ki | Bioorg Med Chem (2011) 19: 5023-5030 [PMID:21757360] |
ChEMBL | Inhibition of human carbonic anhydrase 1-catalyzed CO2 hydration activity by stopped flow assay | B | 4.3 | pKi | 50000 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 5892-5896 [PMID:21852133] |
ChEMBL | Inhibition of human recombinant carbonic anhydrase 1 after 15 mins by stopped flow CO2 hydration assay | B | 4.3 | pKi | 50000 | nM | Ki | Bioorg Med Chem (2012) 20: 1403-1410 [PMID:22285172] |
ChEMBL | Inhibition of human recombinant full length CA1 pre-incubated for 15 mins by stopped-flow CO2 hydration method | B | 4.3 | pKi | 50000 | nM | Ki | J Med Chem (2012) 55: 9619-9629 [PMID:23067387] |
ChEMBL | Inhibition of human recombinant carbonic anhydrase 1 preincubated for 15 mins by stopped-flow CO2 hydrase assay | B | 4.3 | pKi | 50000 | nM | Ki | J Med Chem (2012) 55: 10742-10748 [PMID:23181552] |
ChEMBL | Inhibition of human recombinant carbonic anhydrase 1 by stopped flow CO2 hydration assay | B | 4.3 | pKi | 50000 | nM | Ki | J Med Chem (2013) 56: 1761-1771 [PMID:23391336] |
ChEMBL | Inhibition of human recombinant carbonic anhydrase 1 preincubated for 15 mins by CO2 hydration stopped-flow assay | B | 4.3 | pKi | 50000 | nM | Ki | Bioorg Med Chem (2013) 21: 1534-1538 [PMID:22883029] |
ChEMBL | Inhibition of human cytosolic carbonic anhydrase 1 preincubated for 15 mins by stopped flow CO2 hydration assay | B | 4.3 | pKi | 50000 | nM | Ki | Bioorg Med Chem (2013) 21: 5168-5174 [PMID:23867389] |
ChEMBL | Inhibition of human cytosolic carbonic anhydrase 1 preincubated for 15 mins at room temperature followed by 72 hrs at 4 degC by stopped flow CO2 hydration assay | B | 4.3 | pKi | 50000 | nM | Ki | Bioorg Med Chem (2013) 21: 5973-5982 [PMID:23965175] |
ChEMBL | Inhibition of human cytosolic carbonic anhydrase 1 by stopped-flow CO2 hydration assay | B | 4.3 | pKi | 50000 | nM | Ki | Bioorg Med Chem (2014) 22: 1586-1595 [PMID:24513184] |
ChEMBL | Inhibition of human carbonic anhydrase-1 by stopped-flow CO2 hydration assay | B | 4.3 | pKi | 50000 | nM | Ki | Bioorg Med Chem (2014) 22: 2939-2946 [PMID:24792813] |
ChEMBL | Inhibition of human recombinant Carbonic anhydrase 1 compound preincubated for 15 mins by stopped flow CO2 hydrase assay method | B | 4.3 | pKi | 50000 | nM | Ki | Bioorg Med Chem (2014) 22: 4537-4543 [PMID:25129169] |
ChEMBL | Inhibition of human recombinant carbonic anhydrase 1 by stopped-flow CO2 hydration assay | B | 4.3 | pKi | 50000 | nM | Ki | Bioorg Med Chem (2015) 23: 526-531 [PMID:25533402] |
ChEMBL | Inhibition of human recombinant carbonic anhydrase 1 by stopped flow CO2 hydrase assay | B | 4.3 | pKi | 50000 | nM | Ki | Bioorg Med Chem (2015) 23: 1728-1734 [PMID:25773015] |
ChEMBL | Inhibition of human carbonic anhydrase 1 pre-incubated for 15 mins by stopped-flow CO2 hydration assay | B | 4.3 | pKi | 50000 | nM | Ki | Bioorg Med Chem (2015) 23: 2303-2309 [PMID:25882523] |
ChEMBL | Inhibition of human recombinant CA-1 after 15 mins by stopped-flow CO2 hydrase assay | B | 4.3 | pKi | 50000 | nM | Ki | Bioorg Med Chem (2015) 23: 1828-1840 [PMID:25766630] |
ChEMBL | Inhibition of human CA1 incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay | B | 4.3 | pKi | 50000 | nM | Ki | Bioorg Med Chem Lett (2015) 25: 5485-5489 [PMID:26525863] |
ChEMBL | Inhibition of recombinant human carbonic anhydrase-1 by stopped flow CO2 hydrase assay | B | 4.3 | pKi | 50000 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 401-405 [PMID:26691758] |
ChEMBL | Inhibition of human Carbonic anhydrase1 using CO2 as substrate preincubated for 15 mins by stopped-flow CO2 hydration assay | B | 4.3 | pKi | 50000 | nM | Ki | Bioorg Med Chem (2016) 24: 1115-1120 [PMID:26850377] |
ChEMBL | Inhibition of human carbonic anhydrase 1 incubated for 15 mins by stopped-flow CO2 hydration assay | B | 4.3 | pKi | 50000 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 1821-1826 [PMID:26920803] |
ChEMBL | Inhibition of recombinant human carbonic anhydrase 1 assessed as reduction in CO2 hydration preincubated for 15 mins followed by CO2 addition measured for 10 to 100 sec by Line-Weaver Burk plot analysis | B | 4.3 | pKi | 50000 | nM | Ki | Bioorg Med Chem Lett (2017) 27: 490-495 [PMID:28025002] |
ChEMBL | Inhibitory activity against human carbonic anhydrase I (hCAI) | B | 4.3 | pKi | 50000 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 1149-1154 [PMID:15686931] |
ChEMBL | Inhibition of human carbonic anhydrase-1 assessed as reduction in CO2 hydration preincubated for 15 mins followed by CO2 addition measured for 10 to 100 secs by stopped-flow assay | B | 4.3 | pKi | 50000 | nM | Ki | Bioorg Med Chem (2017) 25: 3555-3561 [PMID:28511911] |
ChEMBL | Inhibition of recombinant human cytosolic carbonic anhydrase 1 assessed as inhibition of CO2 hydration preincubated for 15 mins prior to testing by phenol red based stopped-flow CO2 hydration assay | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem (2017) 25: 2210-2217 [PMID:28256371] |
ChEMBL | Inhibitory activity against human carbonic anhydrase I was determined | B | 4.3 | pIC50 | 50000 | nM | IC50 | J Med Chem (2004) 47: 550-557 [PMID:14736236] |
ChEMBL | Inhibitory activity of compound against human carbonic anhydrase I | F | 4.3 | pIC50 | 50000 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 337-341 [PMID:14698154] |
ChEMBL | Inhibitory concentration against carbonic anhydrase I | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2005) 48: 6523-6543 [PMID:16220969] |
carbonic anhydrase 2/Carbonic anhydrase II in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL205] [GtoPdb: 3092] [UniProtKB: P00918] | ||||||||
ChEMBL | Inhibitory activity against human carbonic anhydrase II at 0.01 uM | B | 4.68 | pKi | 21000 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 6001-6006 [PMID:15546717] |
ChEMBL | Inhibition of human wild type carbonic anhydrase 2 Asn67Ile mutant expressed in Escherichia coli after 15 mins preincubation by stopped flow CO2 hydration assay | B | 6.38 | pKi | 421 | nM | Ki | Bioorg Med Chem (2012) 20: 2208-2213 [PMID:22386980] |
ChEMBL | Inhibition of human wild type carbonic anhydrase 2 Gln92Val mutant expressed in Escherichia coli after 15 mins preincubation by stopped flow CO2 hydration assay | B | 7.11 | pKi | 76.8 | nM | Ki | Bioorg Med Chem (2012) 20: 2208-2213 [PMID:22386980] |
ChEMBL | Inhibition of human recombinant carbonic anhydrase 2 by stopped flow CO2 hydration method | B | 7.68 | pKi | 21 | nM | Ki | J Med Chem (2009) 52: 2226-2232 [PMID:19317447] |
ChEMBL | Inhibition of human recombinant CA2 by stopped-flow CO2 hydrase assay | B | 7.68 | pKi | 21 | nM | Ki | Bioorg Med Chem (2009) 17: 1158-1163 [PMID:19124253] |
ChEMBL | Inhibition of human recombinant carbonic anhydrase 2 by stopped flow CO2 hydrase assay | B | 7.68 | pKi | 21 | nM | Ki | J Med Chem (2009) 52: 646-654 [PMID:19193158] |
ChEMBL | Inhibition of human recombinant carbonic anhydrase 2 by stopped flow CO2 hydration assay | B | 7.68 | pKi | 21 | nM | Ki | J Med Chem (2009) 52: 3116-3120 [PMID:19338333] |
ChEMBL | Inhibition of Helicobacter pylori beta-carbonic anhydrase by stopped-flow CO2 hydration assay | B | 7.68 | pKi | 21 | nM | Ki | Bioorg Med Chem (2009) 17: 4503-4509 [PMID:19450983] |
ChEMBL | Inhibition of human recombinant CA2 by stopped-flow CO2 assay | B | 7.68 | pKi | 21 | nM | Ki | Bioorg Med Chem (2009) 17: 5054-5058 [PMID:19520577] |
ChEMBL | Inhibition of human recombinant CA2 by stopped-flow hydration assay | B | 7.68 | pKi | 21 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 6649-6654 [PMID:19846301] |
ChEMBL | Inhibition of human recombinant carbonic anhydrase 2 after 15 mins by stopped-flow CO2 hydration assay | B | 7.68 | pKi | 21 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 4376-4381 [PMID:20605094] |
ChEMBL | Inhibition of human recombinant carbonic anhydrase 2 after 15 mins by CO2 hydration method | B | 7.68 | pKi | 21 | nM | Ki | Bioorg Med Chem (2010) 18: 5498-5503 [PMID:20624682] |
ChEMBL | Inhibition of human recombinant CA2 by stopped-flow CO2 hydration assay | B | 7.68 | pKi | 21 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 710-714 [PMID:21208801] |
ChEMBL | Inhibition of human carbonic anhydrase II by spectrophotometry at pH 7.5 | B | 7.68 | pKi | 21 | nM | Ki | Bioorg Med Chem (2011) 19: 1172-1178 [PMID:21251841] |
ChEMBL | Inhibition of human recombinant carbonic anhydrase 2 at pH 7.5 by stopped flow CO2 hydration assay | B | 7.68 | pKi | 21 | nM | Ki | Bioorg Med Chem (2011) 19: 5023-5030 [PMID:21757360] |
ChEMBL | Inhibition of human carbonic anhydrase 2-catalyzed CO2 hydration activity by stopped flow assay | B | 7.68 | pKi | 21 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 5892-5896 [PMID:21852133] |
ChEMBL | Inhibition of human recombinant carbonic anhydrase 2 after 15 mins by stopped flow CO2 hydration assay | B | 7.68 | pKi | 21 | nM | Ki | Bioorg Med Chem (2012) 20: 1403-1410 [PMID:22285172] |
ChEMBL | Inhibition of human carbonic anhydrase 2 preincubated for 15 mins measured for 10 to 100 sec by stopped-flow method | B | 7.68 | pKi | 21 | nM | Ki | J Med Chem (2012) 55: 3513-3520 [PMID:22424239] |
ChEMBL | Inhibition of human recombinant full length CA2 pre-incubated for 15 mins by stopped-flow CO2 hydration method | B | 7.68 | pKi | 21 | nM | Ki | J Med Chem (2012) 55: 9619-9629 [PMID:23067387] |
ChEMBL | Inhibition of human recombinant carbonic anhydrase 2 preincubated for 15 mins by stopped-flow CO2 hydrase assay | B | 7.68 | pKi | 21 | nM | Ki | J Med Chem (2012) 55: 10742-10748 [PMID:23181552] |
ChEMBL | Inhibition of human recombinant carbonic anhydrase 2 by stopped flow CO2 hydration assay | B | 7.68 | pKi | 21 | nM | Ki | J Med Chem (2013) 56: 1761-1771 [PMID:23391336] |
ChEMBL | Inhibition of human recombinant carbonic anhydrase 2 preincubated for 15 mins by CO2 hydration stopped-flow assay | B | 7.68 | pKi | 21 | nM | Ki | Bioorg Med Chem (2013) 21: 1534-1538 [PMID:22883029] |
ChEMBL | Inhibition of human cytosolic carbonic anhydrase 2 preincubated for 15 mins by stopped flow CO2 hydration assay | B | 7.68 | pKi | 21 | nM | Ki | Bioorg Med Chem (2013) 21: 5168-5174 [PMID:23867389] |
ChEMBL | Inhibition of human cytosolic carbonic anhydrase 2 preincubated for 15 mins at room temperature followed by 72 hrs at 4 degC by stopped flow CO2 hydration assay | B | 7.68 | pKi | 21 | nM | Ki | Bioorg Med Chem (2013) 21: 5973-5982 [PMID:23965175] |
ChEMBL | Inhibition of human recombinant carbonic anhydrase 2 preincubated for 15 mins by stopped flow CO2 hydration assay | B | 7.68 | pKi | 21 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 275-279 [PMID:24314394] |
ChEMBL | Inhibition of human cytosolic carbonic anhydrase 2 by stopped-flow CO2 hydration assay | B | 7.68 | pKi | 21 | nM | Ki | Bioorg Med Chem (2014) 22: 1586-1595 [PMID:24513184] |
ChEMBL | Inhibition of human carbonic anhydrase-2 by stopped-flow CO2 hydration assay | B | 7.68 | pKi | 21 | nM | Ki | Bioorg Med Chem (2014) 22: 2939-2946 [PMID:24792813] |
ChEMBL | Inhibition of human recombinant Carbonic anhydrase 2 compound preincubated for 15 mins by stopped flow CO2 hydrase assay method | B | 7.68 | pKi | 21 | nM | Ki | Bioorg Med Chem (2014) 22: 4537-4543 [PMID:25129169] |
ChEMBL | Inhibition of human recombinant carbonic anhydrase 2 by stopped-flow CO2 hydration assay | B | 7.68 | pKi | 21 | nM | Ki | Bioorg Med Chem (2015) 23: 526-531 [PMID:25533402] |
ChEMBL | Inhibition of human recombinant carbonic anhydrase 2 by stopped flow CO2 hydrase assay | B | 7.68 | pKi | 21 | nM | Ki | Bioorg Med Chem (2015) 23: 1728-1734 [PMID:25773015] |
ChEMBL | Inhibition of human carbonic anhydrase 2 pre-incubated for 15 mins by stopped-flow CO2 hydration assay | B | 7.68 | pKi | 21 | nM | Ki | Bioorg Med Chem (2015) 23: 2303-2309 [PMID:25882523] |
ChEMBL | Inhibition of human recombinant CA-2 after 15 mins by stopped-flow CO2 hydrase assay | B | 7.68 | pKi | 21 | nM | Ki | Bioorg Med Chem (2015) 23: 1828-1840 [PMID:25766630] |
ChEMBL | Inhibition of human recombinant carbonic anhydrase-2 by stopped flow CO2 hydrase assay method | B | 7.68 | pKi | 21 | nM | Ki | Bioorg Med Chem Lett (2015) 25: 3550-3555 [PMID:26174556] |
ChEMBL | Inhibition of human CA2 incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay | B | 7.68 | pKi | 21 | nM | Ki | Bioorg Med Chem Lett (2015) 25: 5485-5489 [PMID:26525863] |
ChEMBL | Inhibition of recombinant human carbonic anhydrase-2 by stopped flow CO2 hydrase assay | B | 7.68 | pKi | 21 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 401-405 [PMID:26691758] |
ChEMBL | Inhibition of human Carbonic anhydrase2 using CO2 as substrate preincubated for 15 mins by stopped-flow CO2 hydration assay | B | 7.68 | pKi | 21 | nM | Ki | Bioorg Med Chem (2016) 24: 1115-1120 [PMID:26850377] |
ChEMBL | Inhibition of human carbonic anhydrase 2 preincubated for 15 mins by CO2 hydrase stopped flow assay | B | 7.68 | pKi | 21 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 1253-1259 [PMID:26832216] |
ChEMBL | Inhibition of human carbonic anhydrase 2 incubated for 15 mins by stopped-flow CO2 hydration assay | B | 7.68 | pKi | 21 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 1821-1826 [PMID:26920803] |
ChEMBL | Inhibition of human carbonic anhydrase 2 assessed as reduction in CO2 hydration preincubated for 15 mins followed by CO2 addition measured for 10 to 100 sec by Line-Weaver Burk plot analysis | B | 7.68 | pKi | 21 | nM | Ki | Bioorg Med Chem Lett (2017) 27: 490-495 [PMID:28025002] |
ChEMBL | Inhibition of recombinant human carbonic anhydrase 2 assessed as inhibition of CO2 hydration preincubated for 15 mins prior to testing by phenol red based stopped-flow CO2 hydration assay | B | 7.68 | pKi | 21 | nM | Ki | Bioorg Med Chem (2017) 25: 2210-2217 [PMID:28256371] |
ChEMBL | Inhibition of human carbonic anhydrase-2 assessed as reduction in CO2 hydration preincubated for 15 mins followed by CO2 addition measured for 10 to 100 secs by stopped-flow assay | B | 7.68 | pKi | 21 | nM | Ki | Bioorg Med Chem (2017) 25: 3555-3561 [PMID:28511911] |
ChEMBL | Inhibition of human cytosolic carbonic anhydrase 2 preincubated for 15 mins by stop flow CO2 hydrase assay | B | 7.68 | pKi | 21 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 4184-4190 [PMID:27485387] |
ChEMBL | Inhibitory activity against human carbonic anhydrase II (hCAII) | B | 7.68 | pKi | 21 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 1149-1154 [PMID:15686931] |
ChEMBL | Binding affinity to human recombinant CA2 assessed as inhibition constant incubated for 15 mins prior to testing by phenol red based stopped-flow CO2 hydration assay | B | 7.68 | pKi | 21 | nM | Ki | Eur J Med Chem (2021) 209: 112923-112923 [PMID:33121862] |
ChEMBL | Inhibition of cloned human carbonic anhydrase II | B | 7.68 | pKi | 21 | nM | Ki | J Med Chem (2005) 48: 5721-5727 [PMID:16134940] |
ChEMBL | Inhibitory activity against cloned human CA2 | B | 7.68 | pKi | 21 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 437-442 [PMID:16290146] |
ChEMBL | DRUGMATRIX: Carbonic Anhydrase II enzyme inhibition (substrate: 4-Nitrophenyl acetate (4-NPA)) | B | 6.74 | pIC50 | 181 | nM | IC50 | DrugMatrix in vitro pharmacology data |
ChEMBL | Inhibitory activity against human carbonic anhydrase II was determined | B | 7.68 | pIC50 | 21 | nM | IC50 | J Med Chem (2004) 47: 550-557 [PMID:14736236] |
ChEMBL | Inhibitory activity of compound against human carbonic anhydrase II | F | 7.68 | pIC50 | 21 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 337-341 [PMID:14698154] |
ChEMBL | Inhibitory concentration against carbonic anhydrase II | B | 7.68 | pIC50 | 21 | nM | IC50 | J Med Chem (2005) 48: 6523-6543 [PMID:16220969] |
Carbonic anhydrase III in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2885] [UniProtKB: P07451] | ||||||||
ChEMBL | Inhibition of human recombinant carbonic anhydrase 3 after 15 mins by stopped-flow CO2 hydration assay | B | 4.15 | pKi | 70000 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 4376-4381 [PMID:20605094] |
ChEMBL | Inhibition of human recombinant full length CA3 pre-incubated for 15 mins by stopped-flow CO2 hydration method | B | 5.13 | pKi | 7400 | nM | Ki | J Med Chem (2012) 55: 9619-9629 [PMID:23067387] |
carbonic anhydrase 4/Carbonic anhydrase IV in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3729] [GtoPdb: 2599] [UniProtKB: P22748] | ||||||||
ChEMBL | Inhibitory activity against human carbonic anhydrase IV (hCAIV) | B | 6.06 | pKi | 880 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 1149-1154 [PMID:15686931] |
ChEMBL | Inhibition of human recombinant carbonic anhydrase 4 after 15 mins by stopped-flow CO2 hydration assay | B | 6.06 | pKi | 880 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 4376-4381 [PMID:20605094] |
ChEMBL | Inhibition of human recombinant full length CA4 pre-incubated for 15 mins by stopped-flow CO2 hydration method | B | 6.06 | pKi | 880 | nM | Ki | J Med Chem (2012) 55: 9619-9629 [PMID:23067387] |
ChEMBL | Inhibition of recombinant human membrane-associated carbonic anhydrase 4 assessed as inhibition of CO2 hydration preincubated for 15 mins prior to testing by phenol red based stopped-flow CO2 hydration assay | B | 6.54 | pKi | 290 | nM | Ki | Bioorg Med Chem (2017) 25: 2210-2217 [PMID:28256371] |
ChEMBL | Binding affinity to human recombinant CA4 assessed as inhibition constant incubated for 15 mins prior to testing by phenol red based stopped-flow CO2 hydration assay | B | 6.54 | pKi | 290 | nM | Ki | Eur J Med Chem (2021) 209: 112923-112923 [PMID:33121862] |
Carbonic anhydrase IV in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL281] [UniProtKB: Q95323] | ||||||||
ChEMBL | Inhibitory activity against bovine carbonic anhydrase IV (bCAIV) | B | 6.54 | pKi | 290 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 1149-1154 [PMID:15686931] |
ChEMBL | Inhibitory activity against CA4 isolated from bovine lung microsomes | B | 6.54 | pKi | 290 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 437-442 [PMID:16290146] |
ChEMBL | Inhibitory activity against bovine carbonic anhydrase IV was determined | B | 6.54 | pIC50 | 290 | nM | IC50 | J Med Chem (2004) 47: 550-557 [PMID:14736236] |
ChEMBL | Inhibitory activity of compound against bovine carbonic anhydrase IV | F | 6.54 | pIC50 | 290 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 337-341 [PMID:14698154] |
carbonic anhydrase 9/Carbonic anhydrase IX in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3594] [GtoPdb: 3055] [UniProtKB: Q16790] | ||||||||
ChEMBL | Inhibitory activity against human carbonic anhydrase IX at 0.09 uM | B | 4.8 | pKi | 16000 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 6001-6006 [PMID:15546717] |
ChEMBL | Inhibition of recombinant human tumor-associated carbonic anhydrase 9 assessed as inhibition of CO2 hydration preincubated for 15 mins prior to testing by phenol red based stopped-flow CO2 hydration assay | B | 7.7 | pKi | 20 | nM | Ki | Bioorg Med Chem (2017) 25: 2210-2217 [PMID:28256371] |
ChEMBL | Inhibitory activity against cloned human CA9 | B | 7.8 | pKi | 16 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 437-442 [PMID:16290146] |
ChEMBL | Inhibition of human recombinant carbonic anhydrase 9 catalytic domain by stopped flow CO2 hydrase assay | B | 7.8 | pKi | 16 | nM | Ki | J Med Chem (2009) 52: 646-654 [PMID:19193158] |
ChEMBL | Inhibition of human recombinant carbonic anhydrase 9 after 15 mins by stopped-flow CO2 hydration assay | B | 7.8 | pKi | 16 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 4376-4381 [PMID:20605094] |
ChEMBL | Inhibition of human carbonic anhydrase 9-catalyzed CO2 hydration activity by stopped flow assay | B | 7.8 | pKi | 16 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 5892-5896 [PMID:21852133] |
ChEMBL | Inhibition of human recombinant CA9 catalytic domain pre-incubated for 15 mins by stopped-flow CO2 hydration method | B | 7.8 | pKi | 16 | nM | Ki | J Med Chem (2012) 55: 9619-9629 [PMID:23067387] |
ChEMBL | Inhibition of human membrane bound carbonic anhydrase 9 preincubated for 15 mins at room temperature followed by 72 hrs at 4 degC by stopped flow CO2 hydration assay | B | 7.8 | pKi | 16 | nM | Ki | Bioorg Med Chem (2013) 21: 5973-5982 [PMID:23965175] |
ChEMBL | Inhibition of human transmembrane carbonic anhydrase 9 by stopped-flow CO2 hydration assay | B | 7.8 | pKi | 16 | nM | Ki | Bioorg Med Chem (2014) 22: 1586-1595 [PMID:24513184] |
ChEMBL | Inhibition of human recombinant CA-9 after 15 mins by stopped-flow CO2 hydrase assay | B | 7.8 | pKi | 16 | nM | Ki | Bioorg Med Chem (2015) 23: 1828-1840 [PMID:25766630] |
ChEMBL | Inhibition of human recombinant CA9 | B | 7.8 | pKi | 16 | nM | Ki | Eur J Med Chem (2020) 205: 112666-112666 [PMID:32795767] |
ChEMBL | Inhibition of catalytic domain of human recombinant carbonic anhydrase IX | B | 7.8 | pKi | 16 | nM | Ki | J Med Chem (2005) 48: 5721-5727 [PMID:16134940] |
ChEMBL | Binding affinity to human recombinant CA9 assessed as inhibition constant incubated for 15 mins prior to testing by phenol red based stopped-flow CO2 hydration assay | B | 7.83 | pKi | 14.8 | nM | Ki | Eur J Med Chem (2021) 209: 112923-112923 [PMID:33121862] |
ChEMBL | Inhibitory activity against human carbonic anhydrase IX was determined | B | 7.8 | pIC50 | 16 | nM | IC50 | J Med Chem (2004) 47: 550-557 [PMID:14736236] |
ChEMBL | Inhibitory concentration against carbonic anhydrase IX | B | 7.8 | pIC50 | 16 | nM | IC50 | J Med Chem (2005) 48: 6523-6543 [PMID:16220969] |
carbonic anhydrase 5A/Carbonic anhydrase VA in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4789] [GtoPdb: 3093] [UniProtKB: P35218] | ||||||||
ChEMBL | Inhibition of human recombinant carbonic anhydrase 5a after 15 mins by stopped-flow CO2 hydration assay | B | 6.1 | pKi | 794 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 4376-4381 [PMID:20605094] |
ChEMBL | Inhibition of human recombinant full length CA5A pre-incubated for 15 mins by stopped-flow CO2 hydration method | B | 6.1 | pKi | 794 | nM | Ki | J Med Chem (2012) 55: 9619-9629 [PMID:23067387] |
Carbonic anhydrase VB in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3969] [UniProtKB: Q9Y2D0] | ||||||||
ChEMBL | Inhibition of human recombinant carbonic anhydrase 5b after 15 mins by stopped-flow CO2 hydration assay | B | 7.03 | pKi | 93 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 4376-4381 [PMID:20605094] |
ChEMBL | Inhibition of human recombinant full length CA5B pre-incubated for 15 mins by stopped-flow CO2 hydration method | B | 7.03 | pKi | 93 | nM | Ki | J Med Chem (2012) 55: 9619-9629 [PMID:23067387] |
Carbonic anhydrase VI in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3025] [UniProtKB: P23280] | ||||||||
ChEMBL | Inhibition of human full length recombinant carbonic anhydrase 6 by stopped flow CO2 hydrase assay | B | 7.03 | pKi | 94 | nM | Ki | J Med Chem (2009) 52: 646-654 [PMID:19193158] |
ChEMBL | Inhibition of human recombinant carbonic anhydrase 6 after 15 mins by stopped-flow CO2 hydration assay | B | 7.03 | pKi | 94 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 4376-4381 [PMID:20605094] |
ChEMBL | Inhibition of human recombinant full length CA6 pre-incubated for 15 mins by stopped-flow CO2 hydration method | B | 7.03 | pKi | 94 | nM | Ki | J Med Chem (2012) 55: 9619-9629 [PMID:23067387] |
carbonic anhydrase 7/Carbonic anhydrase VII in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2326] [GtoPdb: 2749] [UniProtKB: P43166] | ||||||||
ChEMBL | Inhibition of human recombinant carbonic anhydrase 7 after 15 mins by stopped-flow CO2 hydration assay | B | 5.66 | pKi | 2170 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 4376-4381 [PMID:20605094] |
ChEMBL | Inhibition of human recombinant full length CA7 pre-incubated for 15 mins by stopped-flow CO2 hydration method | B | 5.66 | pKi | 2170 | nM | Ki | J Med Chem (2012) 55: 9619-9629 [PMID:23067387] |
ChEMBL | Inhibition of human cytosolic carbonic anhydrase 7 preincubated for 15 mins by stopped flow CO2 hydration assay | B | 5.66 | pKi | 2170 | nM | Ki | Bioorg Med Chem (2013) 21: 5168-5174 [PMID:23867389] |
ChEMBL | Inhibition of human cytosolic carbonic anhydrase 7 preincubated for 15 mins at room temperature followed by 72 hrs at 4 degC by stopped flow CO2 hydration assay | B | 5.66 | pKi | 2170 | nM | Ki | Bioorg Med Chem (2013) 21: 5973-5982 [PMID:23965175] |
ChEMBL | Inhibition of human recombinant carbonic anhydrase 7 preincubated for 15 mins by stopped flow CO2 hydration assay | B | 5.66 | pKi | 2170 | nM | Ki | Eur J Med Chem (2014) 71: 105-111 [PMID:24287559] |
ChEMBL | Inhibition of human recombinant CA-7 after 15 mins by stopped-flow CO2 hydrase assay | B | 5.66 | pKi | 2170 | nM | Ki | Bioorg Med Chem (2015) 23: 1828-1840 [PMID:25766630] |
carbonic anhydrase 12/Carbonic anhydrase XII in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3242] [GtoPdb: 2747] [UniProtKB: O43570] | ||||||||
GtoPdb | - | - | 7.74 | pKi | 18 | nM | Ki | Bioorg Med Chem (2013) 21: 5973-82 [PMID:23965175] |
ChEMBL | Inhibitory activity against cloned human CA12 | B | 7.74 | pKi | 18 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 437-442 [PMID:16290146] |
ChEMBL | Inhibition of human recombinant carbonic anhydrase 12 after 15 mins by stopped-flow CO2 hydration assay | B | 7.74 | pKi | 18 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 4376-4381 [PMID:20605094] |
ChEMBL | Inhibition of human carbonic anhydrase 12-catalyzed CO2 hydration activity by stopped flow assay | B | 7.74 | pKi | 18 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 5892-5896 [PMID:21852133] |
ChEMBL | Inhibition of human recombinant CA12 catalytic domain pre-incubated for 15 mins by stopped-flow CO2 hydration method | B | 7.74 | pKi | 18 | nM | Ki | J Med Chem (2012) 55: 9619-9629 [PMID:23067387] |
ChEMBL | Inhibition of human membrane bound carbonic anhydrase 12 preincubated for 15 mins at room temperature followed by 72 hrs at 4 degC by stopped flow CO2 hydration assay | B | 7.74 | pKi | 18 | nM | Ki | Bioorg Med Chem (2013) 21: 5973-5982 [PMID:23965175] |
ChEMBL | Inhibition of human transmembrane carbonic anhydrase 12 by stopped-flow CO2 hydration assay | B | 7.74 | pKi | 18 | nM | Ki | Bioorg Med Chem (2014) 22: 1586-1595 [PMID:24513184] |
ChEMBL | Inhibition of human recombinant CA-12 after 15 mins by stopped-flow CO2 hydrase assay | B | 7.74 | pKi | 18 | nM | Ki | Bioorg Med Chem (2015) 23: 1828-1840 [PMID:25766630] |
carbonic anhydrase 13/Carbonic anhydrase XIII in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3912] [GtoPdb: 2748] [UniProtKB: Q8N1Q1] | ||||||||
ChEMBL | Inhibition of human recombinant carbonic anhydrase 13 after 15 mins by stopped-flow CO2 hydration assay | B | 7.01 | pKi | 98 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 4376-4381 [PMID:20605094] |
ChEMBL | Inhibition of human recombinant CA13 catalytic domain pre-incubated for 15 mins by stopped-flow CO2 hydration method | B | 7.01 | pKi | 98 | nM | Ki | J Med Chem (2012) 55: 9619-9629 [PMID:23067387] |
carbonic anhydrase 14/Carbonic anhydrase XIV in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3510] [GtoPdb: 2598] [UniProtKB: Q9ULX7] | ||||||||
ChEMBL | Inhibition of human recombinant carbonic anhydrase 14 after 15 mins by stopped-flow CO2 hydration assay | B | 6.16 | pKi | 689 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 4376-4381 [PMID:20605094] |
ChEMBL | Inhibition of human recombinant CA14 catalytic domain pre-incubated for 15 mins by stopped-flow CO2 hydration method | B | 6.16 | pKi | 689 | nM | Ki | J Med Chem (2012) 55: 9619-9629 [PMID:23067387] |
COX-1 /Cyclooxygenase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL221] [GtoPdb: 1375] [UniProtKB: P23219] | ||||||||
ChEMBL | Inhibition of human COX1 expressed in sf9 cells | B | 4 | pIC50 | >100000 | nM | IC50 | J Nat Prod (2005) 68: 1514-1518 [PMID:16252917] |
ChEMBL | Compound was tested for the inhibition of recombinant human Prostaglandin G/H synthase 1 (COX-1) | B | 4 | pIC50 | <100000 | nM | IC50 | J Med Chem (2003) 46: 5484-5504 [PMID:14640557] |
ChEMBL | Inhibition of human platelets COX1 after 2 mins | B | 4 | pIC50 | >100000 | nM | IC50 | Eur J Med Chem (2010) 45: 6027-6038 [PMID:20970223] |
ChEMBL | Inhibition of human platelet COX1 | B | 4 | pIC50 | >100000 | nM | IC50 | Eur J Med Chem (2008) 43: 456-463 [PMID:17532544] |
ChEMBL | Inhibition of COX1 in human OVCAR-3 cells assessed as reduction in PGE2 level incubated for 30 mins by ELISA | B | 4.09 | pIC50 | 80900 | nM | IC50 | ACS Med Chem Lett (2021) 12: 798-804 [PMID:34055228] |
ChEMBL | Inhibition of COX1 (unknown origin) fluorescence based analysis | B | 4.26 | pIC50 | 54550 | nM | IC50 | J Nat Prod (2023) 86: 2592-2619 [PMID:37856864] |
ChEMBL | Inhibition of COX-1 (unknown origin) | B | 4.3 | pIC50 | >50000 | nM | IC50 | Eur J Med Chem (2022) 229: 114085-114085 [PMID:34998058] |
ChEMBL | Inhibition of human COX1 using arachidonic acid assessed as production of PGF2alpha after 5 mins by ELISA | B | 4.36 | pIC50 | 43370 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 3491-3498 [PMID:27349331] |
ChEMBL | Inhibition of COX1 (unknown origin) assessed as reduction in PGE2 level using arachidonic acid as substrate after 5 mins in presence of heme by ELISA | B | 4.44 | pIC50 | 36440 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 3653-3660 [PMID:28720504] |
ChEMBL | Inhibition of human recombinant COX1 by ELISA | B | 4.49 | pIC50 | 32600 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 1947-1951 [PMID:25866240] |
ChEMBL | Inhibition of human COX1 using arachidonic acid as substrate incubated for 2 mins by ELISA method | B | 4.56 | pIC50 | 27830 | nM | IC50 | Eur J Med Chem (2020) 185: 111780-111780 [PMID:31655429] |
ChEMBL | Inhibition of COX-1 (unknown origin) by chemiluminescence assay | B | 4.56 | pIC50 | 27500 | nM | IC50 | Eur J Med Chem (2013) 62: 222-231 [PMID:23353741] |
ChEMBL | Inhibition of COX1 by chemiluminescent enzyme assay | B | 4.56 | pIC50 | 27500 | nM | IC50 | Bioorg Med Chem (2011) 19: 6827-6832 [PMID:22000948] |
ChEMBL | Inhibition of human Prostaglandin G/H synthase 1 | B | 4.57 | pIC50 | 27000 | nM | IC50 | J Med Chem (2002) 45: 1511-1517 [PMID:11906292] |
ChEMBL | Inhibitory effect on Prostaglandin G/H synthase 1 activity was evaluated in human whole blood as TXB2 production | F | 4.58 | pIC50 | 26400 | nM | IC50 | J Med Chem (2002) 45: 1402-1411 [PMID:11906281] |
ChEMBL | Inhibition of COX1 (unknown origin) | B | 4.59 | pIC50 | 25740 | nM | IC50 | Eur J Med Chem (2013) 70: 579-588 [PMID:24211633] |
ChEMBL | Inhibition of COX1 (unknown origin) | B | 4.6 | pIC50 | 25390 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 1017-1025 [PMID:28089698] |
ChEMBL | Inhibition of COX1 (unknown origin) using arachidonic acid as substrate incubated for 10 mins by Ellman's reagent based COX-1/COX-2 ELISA assay | B | 4.61 | pIC50 | 24470 | nM | IC50 | Eur J Med Chem (2019) 169: 168-184 [PMID:30877972] |
ChEMBL | Inhibition of COX1 | B | 4.61 | pIC50 | 24300 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 5634-5637 [PMID:17822894] |
ChEMBL | Inhibition of COX1 in human whole blood assessed as effect on A-23187-stimulated TxB2 production | B | 4.63 | pIC50 | 23470 | nM | IC50 | Bioorg Med Chem (2008) 16: 2697-2706 [PMID:18063374] |
ChEMBL | Colorimetric Assay: The activities of COX-1 and COX-2 were measured after the addition of arachidonic acid and incubation at 25° C. for 5 min by absorbance at 590 nm as specified by the manufacturer. | B | 4.64 | pIC50 | 23000 | nM | IC50 | US-9388139-B2. Derivatives of celeboxib, use thereof and preparation thereof (2016) |
ChEMBL | Inhibition of human Prostaglandin G/H synthase 1 | B | 4.64 | pIC50 | 22900 | nM | IC50 | J Med Chem (2001) 44: 2921-2927 [PMID:11520200] |
ChEMBL | Inhibitory concentration against Prostaglandin G/H synthase 1 | B | 4.64 | pIC50 | 22900 | nM | IC50 | J Med Chem (2001) 44: 3039-3042 [PMID:11520213] |
ChEMBL | In vitro inhibitory concentration of compound required to inhibit Prostaglandin G/H synthase 1 enzyme was determined | B | 4.64 | pIC50 | 22900 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 2753-2756 [PMID:12217369] |
ChEMBL | Inhibition of COX-1 (unknown origin) | B | 4.69 | pIC50 | 20400 | nM | IC50 | Eur J Med Chem (2014) 81: 204-217 [PMID:24836072] |
ChEMBL | Inhibition of COX1 assessed as TBX2 production in human whole blood | F | 4.7 | pIC50 | 20030 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 4440-4443 [PMID:16814546] |
ChEMBL | Inhibition of COX-1 (unknown origin) assessed as reduction in PGH2 formation using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition and measured after 2 mins by enzyme immunoassay | B | 4.7 | pIC50 | 19880 | nM | IC50 | Bioorg Med Chem Lett (2021) 33: 127743-127743 [PMID:33316405] |
ChEMBL | Inhibition of COX1 in human whole blood assessed as inhibition of LPS-stimulated PGE2 production by radioimmunoassay | B | 4.8 | pIC50 | 16000 | nM | IC50 | Bioorg Med Chem (2008) 16: 8072-8081 [PMID:18752957] |
ChEMBL | Inhibition of COX-1 (unknown origin) using arachidonic acid as substrate and measured by fluorometric assay | B | 4.82 | pIC50 | 15275 | nM | IC50 | Eur J Med Chem (2022) 241: 114597-114597 [PMID:35931005] |
GtoPdb | - | - | 4.82 | pIC50 | 15000 | nM | IC50 |
Eur J Med Chem (2017) 141: 306-321 [PMID:29031075]; J Med Chem (1997) 40: 1347-65 [PMID:9135032] |
ChEMBL | Inhibition of COX1 (unknown origin) by solid phase ELISA method | B | 4.82 | pIC50 | 15030 | nM | IC50 | Bioorg Med Chem (2014) 22: 4109-4118 [PMID:24934992] |
ChEMBL | In Vitro activity of compound against human recombinant Prostaglandin G/H synthase 1 | B | 4.82 | pIC50 | 15000 | nM | IC50 | J Med Chem (2000) 43: 775-777 [PMID:10715145] |
ChEMBL | Inhibition of human Prostaglandin G/H synthase 1 | B | 4.82 | pIC50 | 15000 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 1171-1174 [PMID:10328307] |
ChEMBL | In vitro inhibitory concentration required to block recombinant human prostaglandin G/H synthase 1 (COX-1) | B | 4.82 | pIC50 | 15000 | nM | IC50 | J Med Chem (1997) 40: 1347-1365 [PMID:9135032] |
ChEMBL | Inhibition of human COX1 | B | 4.82 | pIC50 | 15000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 993-996 [PMID:21215625] |
ChEMBL | Inhibition of COX1 | B | 4.82 | pIC50 | 15000 | nM | IC50 | J Med Chem (2012) 55: 2287-2300 [PMID:22263894] |
ChEMBL | In Vitro activity of compound against human recombinant Prostaglandin G/H synthase 1 | B | 4.82 | pIC50 | 15000 | nM | IC50 | J Med Chem (2000) 43: 775-777 [PMID:10715145] |
ChEMBL | Inhibition of human COX1 using arachidonic acid as substrate assessed as PGE2 formation incubated for 10 mins prior to substrate addition measured after 10 mins by ELISA | B | 4.82 | pIC50 | 15000 | nM | IC50 | Eur J Med Chem (2014) 76: 494-505 [PMID:24602792] |
ChEMBL | Inhibition of COX1 in human whole blood assessed as reduction in calcium ionophore-stimulated TXB2 production incubated for 1 hr by ELISA | B | 4.83 | pIC50 | 14800 | nM | IC50 | J Med Chem (2021) 64: 11570-11596 [PMID:34279934] |
ChEMBL | Inhibition of COX-1 (unknown origin) using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition measured after 2 mins by ELISA method | B | 4.83 | pIC50 | 14700 | nM | IC50 | Eur J Med Chem (2023) 250: 115180-115180 [PMID:36796297] |
ChEMBL | Inhibitory activity against prostaglandin G/H synthase 1 | B | 4.85 | pIC50 | 14200 | nM | IC50 | J Med Chem (2000) 43: 214-223 [PMID:10649977] |
ChEMBL | Inhibition of COX1 | B | 4.85 | pIC50 | 14000 | nM | IC50 | Eur J Med Chem (2008) 43: 2792-2799 [PMID:18262309] |
ChEMBL | Compound was tested for the inhibition of human Prostaglandin G/H synthase 1 (COX-1) in human whole blood | B | 4.85 | pIC50 | 14000 | nM | IC50 | J Med Chem (2003) 46: 5484-5504 [PMID:14640557] |
ChEMBL | Compound was evaluated for inhibition concentration of prostaglandin G/H synthase 1 in human blood | B | 4.85 | pIC50 | 14000 | nM | IC50 | J Med Chem (2004) 47: 2180-2193 [PMID:15084117] |
ChEMBL | In vitro inhibition of Prostaglandin G/H synthase 1 in human whole blood | B | 4.85 | pIC50 | 14000 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 6049-6052 [PMID:15546727] |
ChEMBL | In vitro inhibitory concentration against Prostaglandin G/H synthase 1 (COX-1) in human whole blood | B | 4.85 | pIC50 | 14000 | nM | IC50 | J Med Chem (2005) 48: 3930-3934 [PMID:15916445] |
ChEMBL | Inhibition of COX1 in human whole blood assessed as TxB2 production after 1 hr | B | 4.85 | pIC50 | 14000 | nM | IC50 | J Med Chem (2007) 50: 1449-1457 [PMID:17335184] |
ChEMBL | Inhibition of COX1 in human whole blood assessed as effect on A23187-induced thromboxane B2 production | B | 4.85 | pIC50 | 14000 | nM | IC50 | J Med Chem (2007) 50: 6367-6382 [PMID:17994684] |
ChEMBL | Inhibition of COX1 expressed in CHO cells assessed as inhibition of arachidonic acid-stimulated PGE2 production by enzyme immunoassay | F | 4.87 | pIC50 | 13500 | nM | IC50 | J Med Chem (2004) 47: 6195-6206 [PMID:15566290] |
ChEMBL | Inhibition of COX1 in human whole blood assessed as inhibition of 12-hydroxyheptadecatrienoic acid production by HPLC method | B | 4.88 | pIC50 | 13100 | nM | IC50 | Bioorg Med Chem (2010) 18: 3910-3924 [PMID:20451397] |
ChEMBL | Inhibition of COX1 in human whole blood assessed as thromboxane B2 production by RIA | B | 4.9 | pIC50 | 12500 | nM | IC50 | J Med Chem (2010) 53: 723-733 [PMID:19957931] |
ChEMBL | Inhibition of COX1 in human whole blood assessed as TXB2 production | B | 4.9 | pIC50 | 12500 | nM | IC50 | J Med Chem (2007) 50: 5403-5411 [PMID:17915854] |
ChEMBL | Inhibition of COX-1 in human whole blood assessed as thromboxane B2 production by RIA | B | 4.9 | pIC50 | 12470 | nM | IC50 | Bioorg Med Chem (2014) 22: 772-786 [PMID:24373735] |
ChEMBL | Inhibition of platelet COX1-mediated TXB2 production in LPS-induced human whole blood after 60 mins by radioimmunoassay | B | 4.9 | pIC50 | 12470 | nM | IC50 | J Med Chem (2011) 54: 7759-7771 [PMID:21992176] |
ChEMBL | In vitro inhibitory activity against recombinant human Prostaglandin G/H synthase 1 | B | 4.97 | pIC50 | 10700 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 1639-1643 [PMID:12729631] |
ChEMBL | Inhibition of COX1 in human whole blood assessed as inhibition of lipopolysaccharide-induced TxB2 production after 30 min by enzyme immunoassay | B | 4.99 | pIC50 | 10194 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 4504-4508 [PMID:19520573] |
ChEMBL | Inhibition of COX-1 by chemiluminescent assay | B | 5 | pIC50 | 10000 | nM | IC50 | Bioorg Med Chem (2012) 20: 6648-6654 [PMID:23062711] |
ChEMBL | Biochemical index for Prostaglandin G/H synthase 1 measured as, thromboxane 2 (TXB2) levels following blood coagulation | B | 5.01 | pIC50 | 9730 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 1745-1748 [PMID:10937738] |
ChEMBL | Inhibition of COX1 (unknown origin) | B | 5.1 | pIC50 | 8000 | nM | IC50 | J Med Chem (2021) 64: 17656-17689 [PMID:34905377] |
ChEMBL | Inhibition of COX1 by enzyme immunoassay | B | 5.11 | pIC50 | 7700 | nM | IC50 | Bioorg Med Chem (2009) 17: 1146-1151 [PMID:19157881] |
ChEMBL | Inhibition of human whole blood COX-1 assessed as production of TXB2 after 24 hrs by EIA | B | 5.15 | pIC50 | 7000 | nM | IC50 | Bioorg Med Chem (2011) 19: 3299-3311 [PMID:21570308] |
ChEMBL | Inhibition of COX1 in human blood assessed as PGE2 level incubated for 15 mins prior to LPS-challenge measured after 24 hrs by enzyme immunoassay | B | 5.18 | pIC50 | 6650 | nM | IC50 | Bioorg Med Chem (2013) 21: 2355-2362 [PMID:23473947] |
ChEMBL | Inhibitory activity against Prostaglandin G/H synthase 1 in human whole blood | B | 5.2 | pIC50 | 6300 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 2207-2212 [PMID:10465547] |
ChEMBL | In vitro inhibitory activity against human whole blood Prostaglandin G/H synthase 1 | B | 5.2 | pIC50 | 6300 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 1773-1778 [PMID:10406640] |
ChEMBL | Inhibitory concentration was measured against Prostaglandin G/H synthase 1 in human whole blood | B | 5.2 | pIC50 | 6300 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 1195-1198 [PMID:12643942] |
ChEMBL | In vitro potency against human Prostaglandin G/H synthase 1 (hCOX-1) in the human whole blood assay. | B | 5.2 | pIC50 | 6300 | nM | IC50 | J Med Chem (1999) 42: 1274-1281 [PMID:10197970] |
ChEMBL | In vitro inhibitory potency against human COX-1 (HWB COX-2) by whole blood assay | B | 5.2 | pIC50 | 6300 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 3181-3186 [PMID:10576684] |
ChEMBL | Inhibition of Prostaglandin G/H synthase 1 in U-937 cells from human histiocytic lymphoma | B | 5.29 | pIC50 | 5100 | nM | IC50 | J Med Chem (2001) 44: 350-361 [PMID:11462976] |
ChEMBL | In vitro inhibitory activity against human Prostaglandin G/H synthase 1 (COX-1) in U-937 cells | B | 5.29 | pIC50 | 5100 | nM | IC50 | J Med Chem (2003) 46: 3463-3475 [PMID:12877584] |
ChEMBL | Inhibition of COX1 in human whole blood assessed as inhibition of calcium ionophore A-23187-stimulated platelet aggregation by measuring TXB2 production | B | 5.59 | pIC50 | 2600 | nM | IC50 | J Med Chem (2004) 47: 6749-6759 [PMID:15615524] |
ChEMBL | Inhibition of COX1 in human whole blood assessed as TXB2 production by enzyme immunoassay | B | 5.59 | pIC50 | 2600 | nM | IC50 | J Med Chem (2009) 52: 5864-5871 [PMID:19791801] |
ChEMBL | Inhibition of COX-1 in human whole blood assessed as thromboxane B2 level in serum after 5 mins by enzyme immunoassay | B | 5.59 | pIC50 | 2600 | nM | IC50 | Eur J Med Chem (2014) 74: 12-22 [PMID:24440378] |
ChEMBL | Inhibition of arachidonic acid induced TXB2 generation in isolated human platelets (Prostaglandin G/H synthase 1 cell assay) | F | 5.7 | pIC50 | 2000 | nM | IC50 | J Med Chem (2002) 45: 1402-1411 [PMID:11906281] |
ChEMBL | In vitro inhibition of cyclooxygenase-1 by inhibition of TXB2 generation with 1 uM arachidonic acid in human platelets | F | 5.73 | pIC50 | 1880 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 533-537 [PMID:11844666] |
ChEMBL | Inhibition of human cyclooxygenase-1 expressed in COS cells | B | 5.77 | pIC50 | 1689 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 5445-5448 [PMID:15454242] |
ChEMBL | Inhibition of human COX1 expressed in african green monkey COS cells assessed as inhibition of arachidonic acid-stimulated PGE2 treated 1 hr before arachidonic acid challenge by enzyme immunoassay | B | 5.77 | pIC50 | 1689 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 4504-4508 [PMID:19520573] |
ChEMBL | Inhibition of human COX1 expressed in baculovirus-infected SF9 cells assessed as inhibition of arachidonic acid-stimulated PGE2 production treated 1 hr before arachidonic acid challenge by enzyme immunoassay | B | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 4504-4508 [PMID:19520573] |
ChEMBL | DRUGMATRIX: Cyclooxygenase COX-1 enzyme inhibition (substrate: Arachidonic acid) | B | 6.14 | pIC50 | 723 | nM | IC50 | DrugMatrix in vitro pharmacology data |
ChEMBL | Inhibition of human recombinant COX1 assessed as reduction in PGF2alpha formation using arachidonic acid as substrate preincubated with enzyme for 10 mins followed by substrate addition for 30 secs and measured after 1 hr by microplate reader based enzyme immunoassay | B | 6.88 | pIC50 | 131.97 | nM | IC50 | Eur J Med Chem (2019) 171: 332-342 [PMID:30928706] |
ChEMBL | Inhibition of COX1 (unknown origin) using arachidonic acid as substrate pretreated for 10 mins followed by substrate addition measured after 2 mins by enzyme-immunoassay | B | 6.9 | pIC50 | 125 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 2377-2383 [PMID:28427813] |
ChEMBL | In vitro inhibitory potency against U-937 microsomal COX-1 | B | 7.3 | pIC50 | 50 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 3181-3186 [PMID:10576684] |
ChEMBL | Inhibition of COX-1 in U-937 (human lymphoma) cell microsomes. | B | 7.3 | pIC50 | 50 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 3187-3192 [PMID:10576685] |
ChEMBL | In vitro potency against human Prostaglandin G/H synthase 1 in U937 microsomes. | B | 7.3 | pIC50 | 50 | nM | IC50 | J Med Chem (1999) 42: 1274-1281 [PMID:10197970] |
ChEMBL | Inhibitory concentration was measured against Prostaglandin G/H synthase 1 in the sensitive U937 microsome assay | B | 7.3 | pIC50 | 50 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 1195-1198 [PMID:12643942] |
ChEMBL | Inhibition of COX1 (unknown origin) | B | 7.89 | pIC50 | 13 | nM | IC50 | Bioorg Med Chem Lett (2023) 80: 129101-129101 [PMID:36481449] |
Cyclooxygenase-1 in Dog (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4133] [UniProtKB: Q8HZR1] | ||||||||
ChEMBL | In vitro inhibitory activity against canine prostaglandin G/H synthase 1. | B | 5.25 | pIC50 | 5570 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 95-98 [PMID:14684306] |
Cyclooxygenase-1 in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2860] [UniProtKB: O62664] | ||||||||
ChEMBL | Inhibition of Bos taurus (bovine) COX-1 by Chemoiluminescence assay | B | 4.61 | pIC50 | 24300 | nM | IC50 | Med Chem Res (2010) 19: 782-793 |
ChEMBL | Inhibition of bovine COX1 assessed as PGE2 formation preincubated for 10 mins by ELISA | B | 4.67 | pIC50 | 21610 | nM | IC50 | Eur J Med Chem (2011) 46: 5763-5768 [PMID:22019186] |
ChEMBL | Inhibition of COX1 in calf endotheliocyte assessed as 6keto-PGF1alpha production pretreated for 20 mins followed by addition of 10 uM arachidonic acid as substrate for 20 mins by radioimmuno assay | B | 5.09 | pIC50 | 8200 | nM | IC50 | Eur J Med Chem (2016) 108: 89-103 [PMID:26638042] |
ChEMBL | Inhibition of COX1 in bovine platelets assessed as formation of 12-hydroxyheptadecatrienoic acid by HPLC | B | 5.1 | pIC50 | 8000 | nM | IC50 | Bioorg Med Chem (2009) 17: 558-568 [PMID:19097798] |
ChEMBL | Inhibition of bovine COX1 by enzyme immunoassay | B | 5.11 | pIC50 | 7700 | nM | IC50 | J Med Chem (2009) 52: 1525-1529 [PMID:19296694] |
Cyclooxygenase-1 in Sheep (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2949] [UniProtKB: P05979] | ||||||||
ChEMBL | Inhibition of ovine COX1 using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition by ELISA | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem (2016) 24: 3818-3828 [PMID:27344214] |
ChEMBL | Inhibition of ovine COX1 using arachidonic acid as substrate pretreated for 5 mins followed by substrate addition and measured after 2 mins by fluorescence based enzyme immunoassay | B | 4 | pIC50 | >100000 | nM | IC50 | Eur J Med Chem (2019) 180: 86-98 [PMID:31301566] |
ChEMBL | Inhibition of ovine COX-1 using arachidonic acid after 5 mins by colorimetric method | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem (2015) 23: 6807-6814 [PMID:26455657] |
ChEMBL | Inhibition of ovine COX1 after 5 mins by enzyme immunoassay | B | 4 | pIC50 | >100000 | nM | IC50 | Eur J Med Chem (2011) 46: 1648-1655 [PMID:21388719] |
ChEMBL | Inhibition of recombinant ovine COX1 | B | 4 | pIC50 | >100000 | nM | IC50 | ACS Med Chem Lett (2021) 12: 798-804 [PMID:34055228] |
ChEMBL | Inhibition of ovine COX1 by enzyme immuno assay | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem (2008) 16: 3907-3916 [PMID:18272371] |
ChEMBL | Inhibition of ovine COX1 after 2 mins by EIA | B | 4 | pIC50 | >100000 | nM | IC50 | Eur J Med Chem (2014) 80: 167-174 [PMID:24780593] |
ChEMBL | Inhibition of ovine COX-1 using arachidonic acid as substrate assessed as production of PGH2-alpha preincubated for 5 mins followed by addition of substrate measured after 2 mins by EIA | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem (2016) 24: 2032-2042 [PMID:27025563] |
ChEMBL | Inhibition of ovine COX1-mediated prostaglandin alpha production by enzyme immuno assay | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 2601-2605 [PMID:23528298] |
ChEMBL | Inhibition of ovine COX-1 using arachidonic acid as substrate preincubated with compound for 5 mins followed by substrate addition and measured after 2 mins by fluorescence spectrum analysis | B | 4 | pIC50 | >100000 | nM | IC50 | J Nat Prod (2023) 86: 958-965 [PMID:36880830] |
ChEMBL | Inhibition of ovine COX-1 assessed as reduction of prostaglandin-G2 to prostaglandin-H2 and oxidation of 10-acetyl-3,7-dihydroxyphenoxazine to resorufin after 5 mins by fluorescence based assay | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 3295-3300 [PMID:26081289] |
ChEMBL | Inhibition of ovine COX1 assessed as inhibition of PGF2alpha production from PGH2 preincubated for 5 mins before arachidonic acid addition measured after 2 mins by enzyme immunoassay | B | 4 | pIC50 | >100000 | nM | IC50 | Eur J Med Chem (2015) 92: 115-123 [PMID:25549551] |
ChEMBL | Inhibition of ovine COX1 preincubated for 5 mins followed by addition of arachidonic acid as substrate measured after 2 mins by enzyme immunoassay | B | 4 | pIC50 | >100000 | nM | IC50 | Eur J Med Chem (2016) 115: 121-131 [PMID:26999325] |
ChEMBL | Inhibition of ovine COX1 pre-incubated for 15 mins followed by addition of heme and fluorometric substrate and further incubated for 15 mins in presence of arachidonic acid by fluorescence based assay | B | 4.09 | pIC50 | 81700 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 2469-2472 [PMID:25980909] |
ChEMBL | Inhibition of ovine COX-1 using arachidonic acid after 15 mins by fluorescence based assay | B | 4.11 | pIC50 | 78400 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 4082-4084 [PMID:26316467] |
ChEMBL | Inhibition of ovine COX1 using fluorometric substrate after 15 mins | B | 4.11 | pIC50 | 78400 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 1986-1989 [PMID:25819096] |
ChEMBL | Inhibition of sheep COX1 using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition and measured after 5 mins by UV-visible spectrophotometric method | B | 4.14 | pIC50 | 72520 | nM | IC50 | Eur J Med Chem (2020) 186: 111863-111863 [PMID:31740050] |
ChEMBL | Inhibition of ovine COX1 assessed as reduction in PGH2-dervied PGF2alpha production using arachidonic acid substrate by enzyme immunoassay | B | 4.3 | pIC50 | >50000 | nM | IC50 | Eur J Med Chem (2014) 87: 868-880 [PMID:24576797] |
ChEMBL | Inhibition of ovine COX1 using arachidonic acid as substrate incubated for 5 mins followed by substrate addition measured after 2 mins by enzyme immunoassay | B | 4.3 | pIC50 | >50000 | nM | IC50 | Medchemcomm (2016) 7: 2309-2327 |
ChEMBL | Inhibition of ovine COX1 assessed as reduction in PGH2 production using arachidonic acid substrate by enzyme immunoassay | B | 4.3 | pIC50 | >50000 | nM | IC50 | Eur J Med Chem (2014) 86: 122-132 [PMID:25147154] |
ChEMBL | Inhibition of ovine COX1 using arachidonic acid as substrate incubated for 10 mins prior to substrate addition measured after 2 mins by enzyme immunoassay | B | 4.3 | pIC50 | >50000 | nM | IC50 | Eur J Med Chem (2014) 76: 482-493 [PMID:24607877] |
ChEMBL | Inhibition of ovine COX1 by enzyme immuno assay | B | 4.3 | pIC50 | >50000 | nM | IC50 | Bioorg Med Chem (2012) 20: 3306-3316 [PMID:22516672] |
ChEMBL | Inhibition of ovine COX1 assessed as PGF2alpha production from PGH2 after 5 mins by enzyme immunoassay | B | 4.3 | pIC50 | >50000 | nM | IC50 | Bioorg Med Chem (2011) 19: 3416-3424 [PMID:21570309] |
ChEMBL | Inhibition of full-length ovine COX-1 using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition and measured after 2 mins by colorimetry | B | 4.32 | pIC50 | 48000 | nM | IC50 | Bioorg Med Chem (2022) 57: 116633-116633 [PMID:35134642] |
ChEMBL | Inhibition of ovine COX1 assessed as PGF2alpha production by enzyme immunoassay | B | 4.46 | pIC50 | 34500 | nM | IC50 | Eur J Med Chem (2012) 47: 111-124 [PMID:22119153] |
ChEMBL | In vitro inhibitory concentration against ovine Prostaglandin G/H synthase 1 | B | 4.48 | pIC50 | 33100 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 4911-4914 [PMID:15341950] |
ChEMBL | Inhibitory activity against ovine COX1 | B | 4.48 | pIC50 | 33100 | nM | IC50 | J Med Chem (2006) 49: 1668-1683 [PMID:16509583] |
ChEMBL | Inhibition of ovine COX1 by enzyme immunoassay | B | 4.48 | pIC50 | 33100 | nM | IC50 | Bioorg Med Chem (2008) 16: 3302-3308 [PMID:18096394] |
ChEMBL | Inhibition of ovine COX1 by enzyme immuno assay | B | 4.48 | pIC50 | 33100 | nM | IC50 | Bioorg Med Chem (2008) 16: 1948-1956 [PMID:18023187] |
ChEMBL | Inhibition of ovine COX1 by enzyme immuno assay | B | 4.48 | pIC50 | 33100 | nM | IC50 | Bioorg Med Chem (2007) 15: 6796-6801 [PMID:17764958] |
ChEMBL | In vitro inhibition of ovine prostaglandin G/H synthase 1 | B | 4.48 | pIC50 | 33100 | nM | IC50 | J Med Chem (2004) 47: 6108-6111 [PMID:15537365] |
ChEMBL | In vitro inhibitory concentration against ovine Cyclooxygenase-1 | B | 4.48 | pIC50 | 33100 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 439-442 [PMID:15603969] |
ChEMBL | Inhibition of ovine COX1 assessed as inhibition of PGF2a formation after 20 mins by Ellman's method | B | 4.48 | pIC50 | 33100 | nM | IC50 | J Med Chem (2010) 53: 3707-3717 [PMID:20387815] |
ChEMBL | Inhibition of ovine Prostaglandin G/H synthase 1 | B | 4.48 | pIC50 | 33100 | nM | IC50 | J Med Chem (2004) 47: 3972-3990 [PMID:15267236] |
ChEMBL | In vitro inhibitory concentration against ovine Cyclooxygenase-1 | B | 4.48 | pIC50 | 33100 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 439-442 [PMID:15603969] |
ChEMBL | Inhibition of ovine COX1 by enzyme-immuno assay | B | 4.48 | pIC50 | 33100 | nM | IC50 | Eur J Med Chem (2009) 44: 3798-3804 [PMID:19457595] |
ChEMBL | Inhibition of ovine COX1 | B | 4.49 | pIC50 | 32000 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 5324-5329 [PMID:25444084] |
ChEMBL | Inhibition of ovine COX1 using arachidonic acid as substrate preincubated for 10 mins before substrate addition measured after 5 mins by EIA | B | 4.52 | pIC50 | >30000 | nM | IC50 | Eur J Med Chem (2014) 80: 47-56 [PMID:24763362] |
ChEMBL | Inhibition of ovine COX1 using arachidonic acid as substrate assessed as production of PGF2alpha preincubated for 10 mins followed by substrate addition measured after 2 mins by EIA in presence of stannous chloride | B | 4.52 | pIC50 | >30000 | nM | IC50 | Bioorg Med Chem (2013) 21: 4581-4590 [PMID:23769654] |
ChEMBL | Inhibition of ovine COX1 using arachidonic acid as substrate assessed as conversion of PGH2 to PGF2alpha after 10 mins by EIA | B | 4.52 | pIC50 | >30000 | nM | IC50 | Bioorg Med Chem (2014) 22: 2080-2089 [PMID:24631365] |
ChEMBL | Inhibition of purified ovine COX1 pre-treated for 1 hr before 10-acetyl-3,7-dihydroxyphenoxazin substrate addition in absence of porcine liver esterase by fluorescence assay | B | 4.52 | pIC50 | 30000 | nM | IC50 | ACS Med Chem Lett (2014) 5: 983-988 [PMID:25221653] |
ChEMBL | Inhibition of ovine COX1 using arachidonic acid as substrate | B | 4.56 | pIC50 | 27250 | nM | IC50 | ACS Med Chem Lett (2014) 5: 512-516 [PMID:24900871] |
ChEMBL | Inhibition of ovine COX1 | B | 4.57 | pIC50 | 26610 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 4440-4443 [PMID:16814546] |
ChEMBL | Inhibition of ovine COX1 using arachidonic acid as substrate incubated for 5 mins followed by substrate addition measured after 2 mins by colorimetric based ELISA | B | 4.6 | pIC50 | >25000 | nM | IC50 | Eur J Med Chem (2018) 158: 134-143 [PMID:30216848] |
ChEMBL | Inhibition of ovine COX1 by chemiluminescent assay | B | 4.61 | pIC50 | 24300 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 3162-3165 [PMID:19447036] |
ChEMBL | Inhibition of ovine COX1 by chemiluminescence assay | B | 4.61 | pIC50 | 24300 | nM | IC50 | Bioorg Med Chem (2009) 17: 5369-5373 [PMID:19596198] |
ChEMBL | Inhibition of ovine COX1 by chemiluminescent enzyme assay | B | 4.61 | pIC50 | 24300 | nM | IC50 | Bioorg Med Chem (2009) 17: 5312-5317 [PMID:19560931] |
ChEMBL | Inhibition of ovine COX1 by enzyme chemiluminescent enzyme assay | B | 4.61 | pIC50 | 24300 | nM | IC50 | Bioorg Med Chem (2010) 18: 1029-1033 [PMID:20061161] |
ChEMBL | Inhibition of ovine COX1 by chemiluminescence assay | B | 4.61 | pIC50 | 24300 | nM | IC50 | Eur J Med Chem (2010) 45: 4013-4017 [PMID:20691338] |
ChEMBL | Inhibition of Ovine COX-1 by chemiluminescent enzyme method | B | 4.61 | pIC50 | 24300 | nM | IC50 | Bioorg Med Chem (2021) 32: 115960-115960 [PMID:33477020] |
ChEMBL | Inhibition of ovine COX1 by chemiluminescent assay | B | 4.61 | pIC50 | 24300 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 1336-1339 [PMID:18226898] |
ChEMBL | Inhibition of Ovis aries (sheep) COX1 using arachidonic acid as substrate using cyclic naphthalene hydrazide by chemiluminescence assay | B | 4.61 | pIC50 | 24300 | nM | IC50 | Med Chem Res (2012) 21: 1869-1875 |
ChEMBL | Inhibition of Ovis aries (sheep) COX1 using arachidonic acid as substrate using cyclic naphthalene hydrazide by chemiluminescence assay | B | 4.61 | pIC50 | 24300 | nM | IC50 | Med Chem Res (2012) 21: 1803-1810 |
ChEMBL | Inhibition of Ovis aries (sheep) cyclooxygenase-1 using arachidonic acid as substrate by chemiluminescent assay | B | 4.61 | pIC50 | 24300 | nM | IC50 | Med Chem Res (2013) 22: 3881-3887 |
ChEMBL | Inhibition of ovine COX1 using arachidonic acid as substrate by chemiluminescence assay | B | 4.61 | pIC50 | 24300 | nM | IC50 | Bioorg Med Chem (2014) 22: 865-873 [PMID:24361187] |
ChEMBL | In vitro inhibitory activity against prostaglandin G/H synthase 1 from ovine | B | 4.64 | pIC50 | 23000 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 1953-1956 [PMID:15050635] |
ChEMBL | Inhibition of Ovis aries (sheep) COX-1 assessed as decrease in PGF2a production from PGH2 upon reduction with stannous chloride using arachidonic acid as substrate pre-incubated with enzyme for 5 min prior to substrate addition by enzyme immunoassay | B | 4.64 | pIC50 | 23000 | nM | IC50 | Med Chem Res (2013) 22: 2493-2504 |
ChEMBL | In vitro inhibition against ovine Prostaglandin G/H synthase 1 | B | 4.64 | pIC50 | 22900 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2205-2209 [PMID:12798335] |
ChEMBL | Inhibition of ram seminal vesicle COX-1 assessed as conversion of arachidonic acid to PGH2 | B | 4.64 | pIC50 | 22900 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 317-324 [PMID:24295787] |
ChEMBL | In vitro inhibitory activity against Prostaglandin G/H synthase 1 (COX-1) | B | 4.64 | pIC50 | 22900 | nM | IC50 | J Med Chem (2003) 46: 4872-4882 [PMID:14584938] |
ChEMBL | Inhibition of ovine COX1 by measuring PGE2 | B | 4.72 | pIC50 | 19030 | nM | IC50 | Bioorg Med Chem (2007) 15: 6109-6118 [PMID:17604631] |
ChEMBL | Inhibition of ovine COX-1 assessed as production of PGE2 using arachidonic acid as a substrate preincubated for 60 mins followed by substrate addition and measured after 2 mins by ELISA analysis | B | 4.78 | pIC50 | 16520 | nM | IC50 | Bioorg Med Chem (2021) 46: 116344-116344 [PMID:34438337] |
ChEMBL | Inhibition of ovine COX-1 assessed as reduction in oxidation of TMPD using arachidonic acid as substrate preincubated for 5 mins followed by substrate and TMPD addition measured after 5 mins by colorimetric assay | B | 4.79 | pIC50 | 16200 | nM | IC50 | Bioorg Med Chem (2017) 25: 665-676 [PMID:27916468] |
ChEMBL | In vitro inhibition against Prostaglandin G/H synthase 1 from ram seminal vesicles | B | 4.81 | pIC50 | 15330 | nM | IC50 | J Med Chem (2003) 46: 3975-3984 [PMID:12954051] |
ChEMBL | Inhibitory activity against prostaglandin G/H synthase 1 (COX-1) | B | 4.82 | pIC50 | 15135.61 | nM | IC50 | J Med Chem (2002) 45: 4816-4827 [PMID:12383007] |
ChEMBL | Inhibition of ovine COX1 by enzyme immunoassay | B | 4.82 | pIC50 | 15130 | nM | IC50 | Bioorg Med Chem (2016) 24: 5626-5632 [PMID:27658794] |
ChEMBL | Inhibition of ovine COX-1 by EIA method | B | 4.82 | pIC50 | 15100 | nM | IC50 | Eur J Med Chem (2019) 183: 111693-111693 [PMID:31539778] |
ChEMBL | Inhibition of ovine COX1 using arachidonic acid as substrate incubated for 10 mins prior to substrate addition measured after 2 mins by spectrophotometry | B | 4.82 | pIC50 | 15000 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 77-82 [PMID:24332492] |
ChEMBL | Inhibition of ovine COX-1 preincubated for 5 mins followed by addition of arachidonic acid as substrate measured after 2 mins by fluorescence analysis | B | 4.82 | pIC50 | 15000 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 1516-1520 [PMID:26898334] |
ChEMBL | Inhibition of ovine COX1 using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition measured after 5 mins by ELISA | B | 4.82 | pIC50 | 15000 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 952-957 [PMID:29426771] |
ChEMBL | Inhibition of ovine COX-1 assessed as decrease in prostaglandin production using arachidonic acid as substrate incubated with enzyme for 10 mins prior to substrate challenge by enzyme immunoassay | B | 4.82 | pIC50 | 15000 | nM | IC50 | Eur J Med Chem (2014) 77: 185-192 [PMID:24631898] |
ChEMBL | Inhibition of ovine COX1 by fluorescence assay | B | 4.82 | pIC50 | 15000 | nM | IC50 | Bioorg Med Chem (2012) 20: 2221-2226 [PMID:22386983] |
ChEMBL | Inhibition of ovine COX1 assessed as reduction in PGH2-derived PGF2alpha using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition measured after 2 mins by enzyme immunoassay | B | 4.82 | pIC50 | 15000 | nM | IC50 | J Med Chem (2016) 59: 3920-3934 [PMID:27019010] |
ChEMBL | Inhibition of ovine COX1 using arachidonic acid as substrate incubated for 1 min prior to substrate addition measured for 25 secs by TMPD-based chromogenic assay | B | 4.82 | pIC50 | 15000 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 6745-6749 [PMID:23010270] |
ChEMBL | Inhibition of ovine COX1 using arachidonic acid as substrate incubated for 10 mins followed by substrate addition and measured after 2 mins by EIA assay | B | 4.82 | pIC50 | 15000 | nM | IC50 | Bioorg Med Chem (2020) 28: 115246-115246 [PMID:31843462] |
ChEMBL | Inhibition of ovine COX-1 using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition and measured after 2 mins by EIA | B | 4.82 | pIC50 | 15000 | nM | IC50 | J Med Chem (2021) 64: 9550-9566 [PMID:34137625] |
ChEMBL | Inhibition of ovine COX-1 assessed as PGF2alpha formation using arachidonic acid as substrate pretreated with compound for 20 mins prior to substrate addition by spectrophotometric analysis | B | 4.82 | pIC50 | 15000 | nM | IC50 | Eur J Med Chem (2015) 97: 104-123 [PMID:25956953] |
ChEMBL | Inhibition of ovine COX1 assessed as reduction in PGH2 formation by measuring PGF2alpha by colorimetric assay | B | 4.83 | pIC50 | 14800 | nM | IC50 | Bioorg Med Chem (2017) 25: 5637-5651 [PMID:28916158] |
ChEMBL | Inhibition of ovine COX1 catalytic activity using arachidonic acid as substrate pre-incubated for 10 mins followed by substrate addition and measured after 2 mins by ELISA method | B | 4.83 | pIC50 | 14800 | nM | IC50 | Eur J Med Chem (2019) 167: 562-582 [PMID:30818268] |
ChEMBL | Inhibition of ovine COX -1 by colorimetric inhibitor screening assay kit method | B | 4.83 | pIC50 | 14800 | nM | IC50 | Eur J Med Chem (2019) 167: 161-186 [PMID:30771604] |
ChEMBL | Inhibition of ovine COX1 assessed as reduction in PGF2alpha production using arachidonic acid as substrate by colorimetric method | B | 4.83 | pIC50 | 14800 | nM | IC50 | Eur J Med Chem (2018) 144: 635-650 [PMID:29289887] |
ChEMBL | Inhibition of ovine COX1 by colorimetric analysis | B | 4.83 | pIC50 | 14700 | nM | IC50 | Eur J Med Chem (2020) 200: 112439-112439 [PMID:32485532] |
ChEMBL | Inhibition of ovine COX1 assessed as reduction in PGF2alpha production by ELISA | B | 4.85 | pIC50 | 14000 | nM | IC50 | Eur J Med Chem (2017) 139: 936-946 [PMID:28881288] |
ChEMBL | Inhibition of ovine COX1 peroxidase activity assessed as reduction of PGG2 to PGH2 by measuring oxidized TMPD level by colorimetric assay | B | 4.85 | pIC50 | 14000 | nM | IC50 | Bioorg Med Chem (2014) 22: 2855-2866 [PMID:24751552] |
ChEMBL | Inhibition of ovine COX1 | B | 4.89 | pIC50 | 13000 | nM | IC50 | Bioorg Med Chem (2008) 16: 276-283 [PMID:17937989] |
ChEMBL | In vitro inhibitory activity against prostaglandin G/H synthase 1 from the microsomal fraction of ram seminal vesicles | B | 4.97 | pIC50 | 10700 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 1683-1688 [PMID:15026050] |
ChEMBL | Inhibitory activity against prostaglandin G/H synthase 1 from ram seminal vesicles | B | 4.97 | pIC50 | 10700 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 499-504 [PMID:14698190] |
ChEMBL | Competitive inhibition of ovine COX1 by enzyme immunoassay | B | 5 | pIC50 | 10000 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 2235-2238 [PMID:22341941] |
ChEMBL | Inhibition of ovine COX-1 by fluorescence assay | B | 5.03 | pIC50 | 9400 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1823-1826 [PMID:21316237] |
ChEMBL | Inhibition of sheep COX-1 | B | 5.06 | pIC50 | 8770 | nM | IC50 | Eur J Med Chem (2023) 256: 115443-115443 [PMID:37182334] |
ChEMBL | Inhibition of ovine COX-1 assessed as inhibition of transformation of AA to PGH2 by EIA | B | 5.08 | pIC50 | 8320 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 6922-6925 [PMID:19880317] |
ChEMBL | Inhibition of ovine COX1 assessed as PGF2alpha level by EIA | B | 5.09 | pIC50 | 8100 | nM | IC50 | Bioorg Med Chem (2011) 19: 2074-2083 [PMID:21349729] |
ChEMBL | Inhibition of ovine COX1 by enzyme immuno assay | B | 5.11 | pIC50 | 7700 | nM | IC50 | Bioorg Med Chem (2008) 16: 9694-9698 [PMID:18930406] |
ChEMBL | Inhibition of ovine COX1 using arachidonic acid as substrate by colorimetric enzyme immune assay | B | 5.11 | pIC50 | 7700 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 4358-4369 [PMID:28844389] |
ChEMBL | Inhibition of ovine COX1 by enzyme immunoassay | B | 5.11 | pIC50 | 7700 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 1324-1329 [PMID:20097072] |
ChEMBL | Inhibition of ovine COX1 by enzyme immunoassay | B | 5.11 | pIC50 | 7700 | nM | IC50 | Bioorg Med Chem (2009) 17: 5182-5188 [PMID:19500994] |
ChEMBL | Inhibition of ovine COX1 by enzyme immuno assay | B | 5.11 | pIC50 | 7700 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 6138-6141 [PMID:18945614] |
ChEMBL | Inhibition of ovine COX1 | B | 5.11 | pIC50 | 7700 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 163-168 [PMID:23200247] |
ChEMBL | Inhibition of ovine COX-1 by enzyme immuno assay | B | 5.11 | pIC50 | 7700 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 2154-2159 [PMID:22361134] |
ChEMBL | Inhibition of ovine COX1 by enzyme immuno assay | B | 5.11 | pIC50 | 7700 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 6074-6080 [PMID:21890358] |
ChEMBL | Inhibition of ovine COX1 by enzyme immuno assay | B | 5.11 | pIC50 | 7700 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3951-3956 [PMID:21641217] |
ChEMBL | Inhibition of ovine COX1 by enzyme immuno assay | B | 5.11 | pIC50 | 7700 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 584-588 [PMID:19136259] |
ChEMBL | Inhibition of ovine COX-1 assessed as reduction in PGF2-alpha formation using arachidonic acid as substrate by enzyme immunoassay | B | 5.12 | pIC50 | 7600 | nM | IC50 | Eur J Med Chem (2016) 118: 250-258 [PMID:27131067] |
ChEMBL | Inhibition of ovine COX-1 | B | 5.13 | pIC50 | 7340 | nM | IC50 | RSC Med Chem (2022) 13: 1150-1196 [PMID:36325400] |
ChEMBL | Inhibition of ovine COX1 assessed as PGH2 formation preincubated for 10 mins followed by addition of arachidonic acid as substrate measured after 2 mins by ELISA | B | 5.15 | pIC50 | 7000 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 4757-4762 [PMID:27567369] |
ChEMBL | Inhibition of ovine COX-1 preincubated for 2 mins prior to arachidonic acid addition by enzyme immuno assay | B | 5.16 | pIC50 | 6900 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 5787-5791 [PMID:26546221] |
ChEMBL | Inhibition of sheep COX1 by spectrophotometry | B | 5.16 | pIC50 | 6860 | nM | IC50 | J Med Chem (2010) 53: 6560-6571 [PMID:20804197] |
ChEMBL | Inhibition of ovine COX-1 preincubated for 5 mins followed by arachidonic acid substrate addition by colorimetric enzyme immunoassay | B | 5.17 | pIC50 | 6700 | nM | IC50 | Bioorg Med Chem (2017) 25: 4424-4432 [PMID:28669741] |
ChEMBL | Inhibition of ovine COX1 by enzyme immuno assay | B | 5.17 | pIC50 | 6700 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 406-412 [PMID:26691756] |
ChEMBL | Inhibition of ovine COX1 assessed as reduction in Prostaglandin production by enzyme immunoassay | B | 5.21 | pIC50 | 6200 | nM | IC50 | Bioorg Med Chem (2018) 26: 891-902 [PMID:29373271] |
ChEMBL | Inhibition of ovine COX1 using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition measured after 2 mins by enzyme immunoassay | B | 5.25 | pIC50 | 5640 | nM | IC50 | Eur J Med Chem (2017) 127: 10-21 [PMID:28038322] |
ChEMBL | Inhibition of ovine COX-1 by EIA method | B | 5.26 | pIC50 | 5460 | nM | IC50 | Eur J Med Chem (2020) 200: 112438-112438 [PMID:32485533] |
ChEMBL | Inhibition of ovine purified COX1 after 20 mins | B | 5.4 | pIC50 | >4000 | nM | IC50 | ACS Med Chem Lett (2011) 2: 160-164 [PMID:21318094] |
ChEMBL | Inhibition of ovine COX-1 assessed as decrease in PGH2 production using arachidonic acid as substrate treated with enzyme for 10 mins prior to substrate challenge for 2 mins by enzyme immunoassay | B | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 1958-1962 [PMID:24656662] |
ChEMBL | Inhibition of ovine COX1 by fluorescence assay | B | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem (2013) 21: 4288-4295 [PMID:23706267] |
ChEMBL | Inhibition of ovine COX1 | B | 6.68 | pIC50 | 210 | nM | IC50 | Bioorg Med Chem (2007) 15: 1976-1982 [PMID:17258905] |
ChEMBL | Inhibition of ovine COX-1 using arachidonic acid as substrate by fluorescence assay | B | 7.04 | pIC50 | 91 | nM | IC50 | Eur J Med Chem (2021) 224: 113682-113682 [PMID:34245948] |
ChEMBL | Inhibition of COX1 | B | 8.43 | pIC50 | 3.7 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 4483-4487 [PMID:16806914] |
COX-1 /Cyclooxygenase-1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2649] [GtoPdb: 1375] [UniProtKB: P22437] | ||||||||
ChEMBL | Inhibition of COX1-dependent PGE2 production in LPS-stimulated mouse J774 cells by RIA | B | 5.29 | pIC50 | 5100 | nM | IC50 | J Med Chem (2010) 53: 723-733 [PMID:19957931] |
ChEMBL | In vitro inhibitory activity against Prostaglandin G/H synthase 1 in murine J774 cells | B | 5.29 | pIC50 | 5100 | nM | IC50 | J Med Chem (2005) 48: 3428-3432 [PMID:15857149] |
ChEMBL | Inhibition of COX1 in mouse J774 cells using arachidonic acid as substrate preincubated for 15 mins followed substrate addition and assessed as inhibition of PGE2 production after 30 mins by enzyme immuno-assay (EIA) | B | 5.42 | pIC50 | 3840 | nM | IC50 | Eur J Med Chem (2022) 241: 114615-114615 [PMID:35932568] |
ChEMBL | Inhibition of COX-1-mediated PGE2 production in arachidonic acid-stimulated mouse J774 cells incubated for 15 mins prior to arachidonic acid-challenge by radioimmunoassay | B | 5.42 | pIC50 | 3840 | nM | IC50 | J Med Chem (2011) 54: 7759-7771 [PMID:21992176] |
ChEMBL | Inhibition of COX1 in mouse J774 cells using arachidonic acid as substrate assessed as inhibition of PGE2 production incubated for 15 mins prior to substrate addition measured after 30 mins by radioimmunoassay | B | 5.42 | pIC50 | 3840 | nM | IC50 | Bioorg Med Chem (2013) 21: 3695-3701 [PMID:23680444] |
ChEMBL | Inhibition of COX1 in arachidonic acid-stimulated mouse J774 cells assessed as inhibition of PGE2 production after 15 mins by radioimmunoassay | B | 5.43 | pIC50 | 3700 | nM | IC50 | Bioorg Med Chem (2008) 16: 8072-8081 [PMID:18752957] |
ChEMBL | Inhibition of COX1 in mouse J774 cells assessed as arachidonic acid-induced PGE2 levels by radio immunoassay | B | 5.43 | pIC50 | 3700 | nM | IC50 | J Med Chem (2007) 50: 5403-5411 [PMID:17915854] |
ChEMBL | Tested for inhibition against Prostaglandin G/H synthase 2 from mouse resident macrophages | B | 9.15 | pIC50 | 0.7 | nM | IC50 | J Med Chem (2000) 43: 4582-4593 [PMID:11101350] |
COX-1 /Cyclooxygenase-1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4042] [GtoPdb: 1375] [UniProtKB: Q63921] | ||||||||
ChEMBL | Inhibition of rat seminal vesicle COX-1 using arachidonic acid as substrate assessed as reduction of PGG2 to PGH2 incubated for 1 min prior to substrate addition measured after 25 secs by chromogenic assay | B | 4.82 | pIC50 | 15000 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 2251-2255 [PMID:24745964] |
ChEMBL | In vitro inhibitory concentration against rat prostaglandin G/H synthase 1 | B | 4.85 | pIC50 | 14200 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 2687-2690 [PMID:11591502] |
COX-2 /Cyclooxygenase-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL230] [GtoPdb: 1376] [UniProtKB: P35354] | ||||||||
ChEMBL | Inhibition of human recombinant COX-2 using arachidonic acid as substrate preincubated for 60 mins followed by substrate addition for 2 secs by ADPH based fluorometric analysis | B | 9.33 | pKi | 0.47 | nM | Ki | J Med Chem (2021) 64: 11570-11596 [PMID:34279934] |
ChEMBL | Inhibition of COX-2 (unknown origin) | B | 5.06 | pIC50 | 8770 | nM | IC50 | Eur J Med Chem (2023) 256: 115443-115443 [PMID:37182334] |
ChEMBL | Inhibitory effect on Prostaglandin G/H synthase 2 activity was evaluated in human whole blood as LPS-induced PGE-2 generation | F | 5.44 | pIC50 | 3600 | nM | IC50 | J Med Chem (2002) 45: 1402-1411 [PMID:11906281] |
ChEMBL | Inhibition of COX-2 (unknown origin) incubated for 5 to 10 mins by fluorometric analysis | B | 5.44 | pIC50 | 3600 | nM | IC50 | Eur J Med Chem (2023) 249: 115138-115138 [PMID:36696764] |
ChEMBL | Inhibition of PGHS2 in human whole blood assessed as inhibition of TXB2 production by radioimmunoassay | B | 5.54 | pIC50 | 2900 | nM | IC50 | Bioorg Med Chem (2009) 17: 74-84 [PMID:19059783] |
ChEMBL | Inhibition of COX2 (unknown origin) by colorimetric method | B | 5.58 | pIC50 | 2660 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 1952-1957 [PMID:24661847] |
ChEMBL | Inhibition of human recombinant COX-2 using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition and measured after 2 mins by enzyme immunoassay | B | 5.64 | pIC50 | 2270 | nM | IC50 | RSC Med Chem (2022) 13: 471-496 [PMID:35685617] |
ChEMBL | Inhibition of human COX2 expressed in insect cells using arachidonic acid as substrate pretreated for 3 mins followed by substrate addition measured immediately | B | 5.88 | pIC50 | 1310 | nM | IC50 | J Nat Prod (2017) 80: 2472-2477 [PMID:28885836] |
ChEMBL | Inhibition of recombinant human COX2 using arachidonic acid as substrate pretreated for 5 mins followed by substrate addition and measured after 2 mins by fluorescence based enzyme immunoassay | B | 5.88 | pIC50 | 1310 | nM | IC50 | Eur J Med Chem (2019) 180: 86-98 [PMID:31301566] |
ChEMBL | Activity of COX2 in human heparinized blood assessed as inhibition of LPS-induced PGE2 production after 24 hrs | B | 5.89 | pIC50 | 1300 | nM | IC50 | J Med Chem (2007) 50: 1449-1457 [PMID:17335184] |
ChEMBL | In vitro inhibitory concentration against Prostaglandin G/H synthase 2 (COX-2) in human whole blood | B | 5.92 | pIC50 | 1200 | nM | IC50 | J Med Chem (2005) 48: 3930-3934 [PMID:15916445] |
ChEMBL | Compound was tested for the inhibition of human Prostaglandin G/H synthase 2 (COX-2) in human whole blood | B | 5.92 | pIC50 | 1200 | nM | IC50 | J Med Chem (2003) 46: 5484-5504 [PMID:14640557] |
ChEMBL | Inhibition of COX2 | B | 5.92 | pIC50 | 1200 | nM | IC50 | Eur J Med Chem (2008) 43: 2792-2799 [PMID:18262309] |
ChEMBL | Compound was evaluated for inhibition concentration of prostaglandin G/H synthase 2 in human blood | B | 5.92 | pIC50 | 1200 | nM | IC50 | J Med Chem (2004) 47: 2180-2193 [PMID:15084117] |
ChEMBL | Inhibition of COX2 in human whole blood assessed as effect on LPS-induced thromboxane B2 production | B | 5.92 | pIC50 | 1200 | nM | IC50 | J Med Chem (2007) 50: 6367-6382 [PMID:17994684] |
ChEMBL | In vitro inhibition of Prostaglandin G/H synthase 2 in human whole blood | B | 5.92 | pIC50 | 1200 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 6049-6052 [PMID:15546727] |
ChEMBL | Inhibition of recombinant human COX2 using arachidonic acid as substrate by colorimetric enzyme immune assay | B | 5.94 | pIC50 | 1140 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 4358-4369 [PMID:28844389] |
ChEMBL | Inhibition of human recombinant COX-2 | B | 5.95 | pIC50 | 1110 | nM | IC50 | Eur J Med Chem (2020) 200: 112438-112438 [PMID:32485533] |
ChEMBL | Inhibition of COX-2 (unknown origin) | B | 5.95 | pIC50 | 1110 | nM | IC50 | Eur J Med Chem (2023) 249: 115138-115138 [PMID:36696764] |
ChEMBL | Inhibitory activity against prostaglandin G/H synthase 2 | B | 5.96 | pIC50 | 1100 | nM | IC50 | J Med Chem (2000) 43: 214-223 [PMID:10649977] |
ChEMBL | Inhibition of human recombinant COX2 assessed as decrease in prostaglandin production using arachidonic acid as substrate pretreated for 15 mins followed by substrate addition and measured after 2 mins by enzyme immunoassay | B | 5.97 | pIC50 | 1070 | nM | IC50 | Medchemcomm (2019) 10: 1775-1788 [PMID:31803395] |
ChEMBL | In vitro inhibitory activity against human whole blood Prostaglandin G/H synthase 2 | B | 6 | pIC50 | 1000 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 1773-1778 [PMID:10406640] |
ChEMBL | Inhibitory potency against PGE-2 production in the human whole blood (HWB COX-2) assay | B | 6 | pIC50 | 1000 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 3187-3192 [PMID:10576685] |
ChEMBL | In vitro inhibitory potency against human COX-2 (HWB COX-2) by whole blood assay | B | 6 | pIC50 | 1000 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 3181-3186 [PMID:10576684] |
ChEMBL | In vitro potency against human Prostaglandin G/H synthase 2 in the human whole blood assay. | B | 6 | pIC50 | 1000 | nM | IC50 | J Med Chem (1999) 42: 1274-1281 [PMID:10197970] |
ChEMBL | Inhibition of human COX2 | B | 6 | pIC50 | 1000 | nM | IC50 | Eur J Med Chem (2008) 43: 1152-1159 [PMID:17976864] |
ChEMBL | Inhibitory concentration was measured against Cyclooxygenase-2 in human whole blood | B | 6 | pIC50 | 1000 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 1195-1198 [PMID:12643942] |
ChEMBL | Inhibition of Prostaglandin G/H synthase 2 in human whole blood | B | 6 | pIC50 | 1000 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 2207-2212 [PMID:10465547] |
ChEMBL | Inhibition of human recombinant COX-2 preincubated for 2 mins prior to arachidonic acid addition by enzyme immuno assay | B | 6.05 | pIC50 | 900 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 5787-5791 [PMID:26546221] |
ChEMBL | Inhibition of recombinant human COX2 using arachidonic acid as substrate assessed as decrease in PGF2 production preincubated for 15 mins followed by substrate addition measured after 2 mins by enzyme immunoassay | B | 6.06 | pIC50 | 880 | nM | IC50 | Eur J Med Chem (2017) 127: 972-985 [PMID:27837994] |
ChEMBL | Inhibition of human recombinant COX2 by enzyme immuno assay | B | 6.06 | pIC50 | 870 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 406-412 [PMID:26691756] |
ChEMBL | Inhibition of COX-2 (unknown origin) by EIA kit method | B | 6.06 | pIC50 | 870 | nM | IC50 | Eur J Med Chem (2020) 200: 112438-112438 [PMID:32485533] |
ChEMBL | Inhibition of COX2 in human blood assessed as TxB2 level after 1 hr by enzyme immunoassay | B | 6.06 | pIC50 | 870 | nM | IC50 | Bioorg Med Chem (2013) 21: 2355-2362 [PMID:23473947] |
ChEMBL | Inhibition of human COX-2 preincubated for 5 mins followed by arachidonic acid substrate addition by colorimetric enzyme immunoassay | B | 6.06 | pIC50 | 870 | nM | IC50 | Bioorg Med Chem (2017) 25: 4424-4432 [PMID:28669741] |
ChEMBL | Inhibition of human recombinant COX2 by enzyme immuno assay | B | 6.06 | pIC50 | 870 | nM | IC50 | Medchemcomm (2017) 8: 492-500 [PMID:30108767] |
ChEMBL | Inhibition of COX2 (unknown origin) by EIA | B | 6.08 | pIC50 | 840 | nM | IC50 | Eur J Med Chem (2019) 180: 486-508 [PMID:31330449] |
ChEMBL | Inhibition of recombinant human COX-2 by colorimetric enzyme immunoassay | B | 6.08 | pIC50 | 830 | nM | IC50 | RSC Med Chem (2022) 13: 471-496 [PMID:35685617] |
ChEMBL | Inhibition of COX2 in LPS-stimulated human blood | B | 6.1 | pIC50 | 800 | nM | IC50 | Bioorg Med Chem (2009) 17: 558-568 [PMID:19097798] |
ChEMBL | Inhibition of COX2 in human whole blood assessed as inhibition of 12-hydroxyheptadecatrienoic acid production by HPLC method | B | 6.1 | pIC50 | 800 | nM | IC50 | Bioorg Med Chem (2010) 18: 3910-3924 [PMID:20451397] |
ChEMBL | Inhibition of recombinant human COX-2 using arachidonic acid as substrate preincubated with compound for 5 mins followed by substrate addition and measured after 2 mins by fluorescence spectrum analysis | B | 6.1 | pIC50 | 790 | nM | IC50 | J Nat Prod (2023) 86: 958-965 [PMID:36880830] |
ChEMBL | Inhibition of COX-2 (unknown origin) at 20 uM | B | 6.11 | pIC50 | 780 | nM | IC50 | Eur J Med Chem (2020) 200: 112438-112438 [PMID:32485533] |
ChEMBL | Inhibition of human COX2 using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition measured after 2 mins by enzyme immunoassay | B | 6.11 | pIC50 | 780 | nM | IC50 | Eur J Med Chem (2017) 127: 10-21 [PMID:28038322] |
ChEMBL | Inhibition of human COX2 assessed as reduction in PGF2alpha formation using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition and measured after 2 mins by ELISA | B | 6.15 | pIC50 | 700 | nM | IC50 | Eur J Med Chem (2020) 189: 112066-112066 [PMID:31982653] |
ChEMBL | Inhibition of COX2 (unknown origin) | B | 6.19 | pIC50 | 640 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 1017-1025 [PMID:28089698] |
ChEMBL | In vitro percent inhibition of Prostaglandin G/H synthase 2 (COX-2) in human whole blood was determined | B | 6.22 | pIC50 | 600 | nM | IC50 | J Med Chem (2003) 46: 3463-3475 [PMID:12877584] |
ChEMBL | Inhibition of COX2 in human whole blood assessed as inhibition of TXB2 production by radioimmunoassay | B | 6.27 | pIC50 | 540 | nM | IC50 | Bioorg Med Chem (2008) 16: 8072-8081 [PMID:18752957] |
ChEMBL | Inhibition of COX-2 in human whole blood assessed as prostaglandin E2 production by RIA | B | 6.27 | pIC50 | 540 | nM | IC50 | Bioorg Med Chem (2014) 22: 772-786 [PMID:24373735] |
ChEMBL | Inhibition of COX2-mediated PGE2 production in LPS-induced human whole blood after 60 mins by radioimmunoassay | B | 6.27 | pIC50 | 540 | nM | IC50 | J Med Chem (2011) 54: 7759-7771 [PMID:21992176] |
ChEMBL | Inhibition of COX2 in LPS-induced monocyte assessed as PGE2 production in human whole blood | B | 6.27 | pIC50 | 540 | nM | IC50 | J Med Chem (2007) 50: 5403-5411 [PMID:17915854] |
ChEMBL | Inhibition of COX2 in human whole blood assessed as inhibition of LPS-induced PGE2 production by RIA | B | 6.27 | pIC50 | 540 | nM | IC50 | J Med Chem (2010) 53: 723-733 [PMID:19957931] |
ChEMBL | Biochemical index for Prostaglandin G/H synthase 2 measured as, PGE-2 levels in lipopolysaccharide (LPS)-challenged human whole blood | B | 6.28 | pIC50 | 530 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 1745-1748 [PMID:10937738] |
ChEMBL | Colorimetric Assay: The activities of COX-1 and COX-2 were measured after the addition of arachidonic acid and incubation at 25° C. for 5 min by absorbance at 590 nm as specified by the manufacturer. | B | 6.3 | pIC50 | 500 | nM | IC50 | US-9388139-B2. Derivatives of celeboxib, use thereof and preparation thereof (2016) |
ChEMBL | DRUGMATRIX: Cyclooxygenase COX-2 enzyme inhibition (substrate: Arachidonic acid) | B | 6.32 | pIC50 | 484 | nM | IC50 | DrugMatrix in vitro pharmacology data |
ChEMBL | Inhibition of COX2 in human whole blood assessed as reduction in LPS stimulated PGE2 production incubated for 1 hr by ELISA | B | 6.36 | pIC50 | 440 | nM | IC50 | J Med Chem (2021) 64: 11570-11596 [PMID:34279934] |
ChEMBL | Inhibition of COX2 (unknown origin) assessed as reduction in PGE2 level using arachidonic acid as substrate after 5 mins in presence of heme by ELISA | B | 6.39 | pIC50 | 410 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 3653-3660 [PMID:28720504] |
ChEMBL | Inhibition of human COX-2 using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition and measured after 2 mins by colorimetry | B | 6.4 | pIC50 | 400 | nM | IC50 | Bioorg Med Chem (2022) 57: 116633-116633 [PMID:35134642] |
ChEMBL | Inhibition of COX-2 (unknown origin) | B | 6.42 | pIC50 | 380 | nM | IC50 | Eur J Med Chem (2021) 226: 113865-113865 [PMID:34655985] |
ChEMBL | Inhibition of human COX2 using [14C]arachidonic acid as substrate preincubated for 5 mins followed by substrate addition measured after 45 mins by TLC | B | 6.44 | pIC50 | 360 | nM | IC50 | Bioorg Med Chem (2018) 26: 3731-3762 [PMID:30017112] |
ChEMBL | Inhibition of COX2 (unknown origin) using arachidonic acid as substrate pretreated for 10 mins followed by substrate addition and measured after 2 mins by ELISA | B | 6.44 | pIC50 | 360 | nM | IC50 | Bioorg Med Chem (2018) 26: 4264-4275 [PMID:30031652] |
ChEMBL | Inhibition of COX2 in LPS-stimulated human whole blood assessed as PGE2 production by enzyme immunoassay | B | 6.46 | pIC50 | 350 | nM | IC50 | J Med Chem (2009) 52: 5864-5871 [PMID:19791801] |
ChEMBL | Inhibition of COX2 in human whole blood assessed as inhibition of LPS-stimulated PGE2 production | B | 6.46 | pIC50 | 350 | nM | IC50 | J Med Chem (2004) 47: 6749-6759 [PMID:15615524] |
ChEMBL | Inhibition of COX-2 in human whole blood assessed as PGE2 level in plasma after 5 mins by enzyme immunoassay | B | 6.46 | pIC50 | 350 | nM | IC50 | Eur J Med Chem (2014) 74: 12-22 [PMID:24440378] |
ChEMBL | Inhibition of human recombinant COX-2 assessed as reduction in oxidation of TMPD using arachidonic acid as substrate preincubated for 5 mins followed by substrate and TMPD addition measured after 5 mins by colorimetric assay | B | 6.47 | pIC50 | 340 | nM | IC50 | Bioorg Med Chem (2017) 25: 665-676 [PMID:27916468] |
ChEMBL | Inhibition of COX2 in human whole blood assessed as inhibition of lipopolysaccharide-stimulated PGE2 production after 24 hrs by enzyme immunoassay | B | 6.47 | pIC50 | 336 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 4504-4508 [PMID:19520573] |
ChEMBL | Inhibition of COX2 assessed as LPS-stimulated PGE2 production in human whole blood leukocyte | F | 6.48 | pIC50 | 330 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 4440-4443 [PMID:16814546] |
ChEMBL | Inhibition of human recombinant COX2 expressed in insect cell expression system using TMPD and arachidonic acid as substrate incubated for 1 min prior to substrate addition by spectrophotometry | B | 6.49 | pIC50 | 320 | nM | IC50 | Eur J Med Chem (2013) 70: 579-588 [PMID:24211633] |
ChEMBL | Inhibition of human COX2 using arachidonic acid assessed as production of PGF2alpha after 5 mins by ELISA | B | 6.51 | pIC50 | 310 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 3491-3498 [PMID:27349331] |
GtoPdb | - | - | 6.52 | pIC50 | 300 | nM | IC50 | Eur J Med Chem (2017) 141: 306-321 [PMID:29031075] |
ChEMBL | Inhibition of human recombinant COX2 | B | 6.52 | pIC50 | <300 | nM | IC50 | Eur J Med Chem (2008) 43: 456-463 [PMID:17532544] |
ChEMBL | Inhibition of COX-2 (unknown origin) at 0.5 uM by colorimetric assay | B | 6.52 | pIC50 | 300 | nM | IC50 | Eur J Med Chem (2020) 200: 112438-112438 [PMID:32485533] |
ChEMBL | Inhibition of human COX-2 using [14C]-arachidonic acid as substrate preincubated for 5 mins followed by substrate addition measured after 45 mins by thin layer chromatographic method | B | 6.52 | pIC50 | 300 | nM | IC50 | Eur J Med Chem (2017) 141: 306-321 [PMID:29031075] |
ChEMBL | Inhibition of COX2 in human whole blood assessed as effect on LPS-stimulated PGE2 production | B | 6.52 | pIC50 | 300 | nM | IC50 | Bioorg Med Chem (2008) 16: 2697-2706 [PMID:18063374] |
ChEMBL | Inhibition of human recombinant COX2 after 45 mins | B | 6.52 | pIC50 | <300 | nM | IC50 | Eur J Med Chem (2010) 45: 6027-6038 [PMID:20970223] |
ChEMBL | Inhibition of human recombinant COX2 using arachidonic acid as substrate | B | 6.54 | pIC50 | 290 | nM | IC50 | ACS Med Chem Lett (2014) 5: 512-516 [PMID:24900871] |
ChEMBL | Inhibition of COX-2 (unknown origin) | B | 6.55 | pIC50 | 280 | nM | IC50 | Eur J Med Chem (2022) 229: 114085-114085 [PMID:34998058] |
ChEMBL | Inhibition of human recombinant COX2 after 2 mins by EIA | B | 6.55 | pIC50 | 280 | nM | IC50 | Eur J Med Chem (2014) 80: 167-174 [PMID:24780593] |
ChEMBL | Inhibition of human recombinant COX2 using arachidonic acid as substrate incubated for 10 mins prior to substrate addition measured after 2 mins by enzyme immunoassay | B | 6.55 | pIC50 | 280 | nM | IC50 | Eur J Med Chem (2014) 76: 482-493 [PMID:24607877] |
ChEMBL | Inhibition of COX-2 (unknown origin) | B | 6.57 | pIC50 | 270 | nM | IC50 | Eur J Med Chem (2014) 81: 204-217 [PMID:24836072] |
ChEMBL | Inhibition of COX2 (unknown origin) | B | 6.57 | pIC50 | 270 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127376-127376 [PMID:32738961] |
ChEMBL | Inhibition of recombinant N-terminal His6-tagged human COX-2 expressed in Baculovirus infected Sf21 cells using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition measured after 1 hr | B | 6.59 | pIC50 | 260 | nM | IC50 | Bioorg Med Chem (2018) 26: 5388-5396 [PMID:30293795] |
ChEMBL | Inhibition of COX-2 (unknown origin) | B | 6.59 | pIC50 | 260 | nM | IC50 | Eur J Med Chem (2016) 108: 89-103 [PMID:26638042] |
ChEMBL | Inhibition of COX2 (unknown origin) using arachidonic acid as substrate incubated for 10 mins by Ellman's reagent based COX-1/COX-2 ELISA assay | B | 6.6 | pIC50 | 250 | nM | IC50 | Eur J Med Chem (2019) 169: 168-184 [PMID:30877972] |
ChEMBL | Inhibition of human COX2 using arachidonic acid as substrate incubated for 2 mins by ELISA method | B | 6.6 | pIC50 | 250 | nM | IC50 | Eur J Med Chem (2020) 185: 111780-111780 [PMID:31655429] |
ChEMBL | Inhibition of COX-2 (unknown origin) assessed as reduction in PGH2 formation using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition and measured after 2 mins by enzyme immunoassay | B | 6.62 | pIC50 | 240 | nM | IC50 | Bioorg Med Chem Lett (2021) 33: 127743-127743 [PMID:33316405] |
ChEMBL | Inhibition of human Prostaglandin G/H synthase 2 | B | 6.64 | pIC50 | 230 | nM | IC50 | J Med Chem (2002) 45: 1511-1517 [PMID:11906292] |
ChEMBL | Inhibition of COX2 (unknown origin) | B | 6.66 | pIC50 | 220 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 1909-1912 [PMID:31160177] |
ChEMBL | Inhibition of COX2 assessed as inhibition of PGE2 production using arachidonic acid as substrate after 10 mins by ELISA | B | 6.7 | pIC50 | 200 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 793-796 [PMID:22217871] |
ChEMBL | Inhibition of human whole blood COX-2 assessed as production of PGE2 after 24 hrs by EIA | B | 6.72 | pIC50 | 190 | nM | IC50 | Bioorg Med Chem (2011) 19: 3299-3311 [PMID:21570308] |
ChEMBL | Inhibition of human COX2 assessed as fluorescence by microplate reader | B | 6.8 | pIC50 | 160 | nM | IC50 | Eur J Med Chem (2021) 222: 113564-113564 [PMID:34091208] |
ChEMBL | Inhibition of recombinant human N-terminal His-tagged COX2 expressed in baculovirus infected Sf21 cells assessed as reduction in prostaglandin production by enzyme immunoassay | B | 6.82 | pIC50 | 150 | nM | IC50 | Bioorg Med Chem (2018) 26: 891-902 [PMID:29373271] |
ChEMBL | Inhibition of COX2 | B | 6.82 | pIC50 | 150 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1612-1616 [PMID:21345672] |
ChEMBL | Inhibition of COX2 in human whole blood assessed as inhibition of LPS-induced PGE2 synthesis up to 24 hrs by radioimmunoassay | B | 6.85 | pIC50 | 140 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 5031-5034 [PMID:22749420] |
ChEMBL | Inhibition of COX-2 (unknown origin) using arachidonic acid as substrate measured after 10 mins by fluorometric based multimode microplate reader | B | 6.88 | pIC50 | 132 | nM | IC50 | Eur J Med Chem (2021) 209: 112918-112918 [PMID:33071054] |
ChEMBL | Inhibition of recombinant human COX-2 assessed as reduction of prostaglandin-G2 to prostaglandin-H2 and oxidation of 10-acetyl-3,7-dihydroxyphenoxazine to resorufin after 5 mins by fluorescence based assay | B | 6.89 | pIC50 | 130 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 3295-3300 [PMID:26081289] |
ChEMBL | Inhibition of COX2 by chemiluminescent enzyme assay | B | 6.92 | pIC50 | 120 | nM | IC50 | Bioorg Med Chem (2011) 19: 6827-6832 [PMID:22000948] |
ChEMBL | Inhibition of human recombinant COX2 by enzyme immunoassay | B | 6.92 | pIC50 | 120 | nM | IC50 | Bioorg Med Chem (2009) 17: 5182-5188 [PMID:19500994] |
ChEMBL | Inhibition of human recombinant COX2 by enzyme immunoassay | B | 6.92 | pIC50 | 120 | nM | IC50 | J Med Chem (2009) 52: 1525-1529 [PMID:19296694] |
ChEMBL | Inhibition of human recombinant COX2 by enzyme immuno assay | B | 6.92 | pIC50 | 120 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 584-588 [PMID:19136259] |
ChEMBL | Inhibition of COX-2 (unknown origin) using arachidonic acid as substrate incubated for 5 to 10 mins by fluorometric analysis | B | 6.92 | pIC50 | 120 | nM | IC50 | RSC Med Chem (2022) 13: 471-496 [PMID:35685617] |
ChEMBL | Inhibition of PGE-2 generation in LPS-stimulated human monocytes (Prostaglandin G/H synthase 2 cell assay) | F | 6.92 | pIC50 | 120 | nM | IC50 | J Med Chem (2002) 45: 1402-1411 [PMID:11906281] |
ChEMBL | Inhibition of human recombinant COX2 by enzyme immunoassay | B | 6.92 | pIC50 | 120 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 1324-1329 [PMID:20097072] |
ChEMBL | Inhibition of COX-2 (unknown origin) using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition and measured after 1 hr by spectrophotometer based analysis | B | 6.94 | pIC50 | 115 | nM | IC50 | RSC Med Chem (2022) 13: 471-496 [PMID:35685617] |
ChEMBL | In vitro inhibition of PGE-2 generation by LPS-stimulated monocytes isolated from human blood. | F | 6.96 | pIC50 | 110 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 533-537 [PMID:11844666] |
ChEMBL | Inhibition of COX-2 (unknown origin) using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition and measured after 1 hr by absorbance based analysis | B | 6.96 | pIC50 | 110 | nM | IC50 | RSC Med Chem (2022) 13: 471-496 [PMID:35685617] |
ChEMBL | Inhibition of human recombinant COX-2 assessed as PGF2alpha production by enzyme immunoassay | B | 7 | pIC50 | 100 | nM | IC50 | Eur J Med Chem (2012) 47: 111-124 [PMID:22119153] |
ChEMBL | Inhibition of COX-2 by chemiluminescent assay | B | 7 | pIC50 | 100 | nM | IC50 | Bioorg Med Chem (2012) 20: 6648-6654 [PMID:23062711] |
ChEMBL | Inhibition of COX-2 (unknown origin) by chemiluminescence assay | B | 7 | pIC50 | 100 | nM | IC50 | Eur J Med Chem (2013) 62: 222-231 [PMID:23353741] |
ChEMBL | Inhibition of COX2 human HCA7 cells | B | 7.05 | pIC50 | 90 | nM | IC50 | J Med Chem (2020) 63: 3817-3833 [PMID:31820982] |
ChEMBL | Inhibition of recombinant human COX2 | B | 7.05 | pIC50 | 90 | nM | IC50 | ACS Med Chem Lett (2021) 12: 798-804 [PMID:34055228] |
ChEMBL | Inhibition of COX-2 in human Osteosarcoma cell incubated for 15 mins | B | 7.1 | pIC50 | 80 | nM | IC50 | Eur J Med Chem (2023) 249: 115138-115138 [PMID:36696764] |
ChEMBL | Inhibition of human COX2 expressed in sf9 cells | B | 7.1 | pIC50 | 80 | nM | IC50 | J Nat Prod (2005) 68: 1514-1518 [PMID:16252917] |
ChEMBL | Inhibition of Prostaglandin G/H synthase 2 in 143.98.2 from human osteosarcoma cells | B | 7.1 | pIC50 | 80 | nM | IC50 | J Med Chem (2001) 44: 350-361 [PMID:11462976] |
ChEMBL | In vitro inhibitory activity against human Prostaglandin G/H synthase 2 (COX-2) in 143982 cells | B | 7.1 | pIC50 | 79 | nM | IC50 | J Med Chem (2003) 46: 3463-3475 [PMID:12877584] |
ChEMBL | Inhibition of human recombinant COX-2 assessed as decrease in PGH2 production using arachidonic acid as substrate treated with enzyme for 10 mins prior to substrate challenge for 2 mins by enzyme immunoassay | B | 7.14 | pIC50 | 72 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 1958-1962 [PMID:24656662] |
ChEMBL | In vitro inhibition against human Prostaglandin G/H synthase 2 | B | 7.15 | pIC50 | 70 | nM | IC50 | J Med Chem (2003) 46: 3975-3984 [PMID:12954051] |
ChEMBL | Inhibition of human recombinant COX2 | B | 7.15 | pIC50 | 70 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 163-168 [PMID:23200247] |
ChEMBL | Inhibition of human recombinant COX-2 by enzyme immuno assay | B | 7.15 | pIC50 | 70 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 2154-2159 [PMID:22361134] |
ChEMBL | Inhibition of COX2 by enzyme immunoassay | B | 7.15 | pIC50 | 70 | nM | IC50 | Bioorg Med Chem (2009) 17: 1146-1151 [PMID:19157881] |
ChEMBL | Inhibition of COX-2 (unknown origin) | B | 7.15 | pIC50 | 70 | nM | IC50 | Eur J Med Chem (2020) 200: 112438-112438 [PMID:32485533] |
ChEMBL | Inhibition of human recombinant COX-2 by enzyme immunoassay | B | 7.15 | pIC50 | 70 | nM | IC50 | Bioorg Med Chem (2014) 22: 2529-2534 [PMID:24650702] |
ChEMBL | Inhibition of human COX2 assessed as reduction in PGE2 production incubated for 2 mins using arachidonic acid substrate by enzyme immuno assay | B | 7.15 | pIC50 | 70 | nM | IC50 | Medchemcomm (2017) 8: 492-500 [PMID:30108767] |
ChEMBL | Inhibition of human COX2 | B | 7.15 | pIC50 | 70 | nM | IC50 | J Med Chem (2020) 63: 3817-3833 [PMID:31820982] |
ChEMBL | Inhibition of human recombinant COX2 by enzyme immuno assay | B | 7.15 | pIC50 | 70 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3951-3956 [PMID:21641217] |
ChEMBL | Inhibition of human cyclooxygenase-2 expressed in COS cells | B | 7.17 | pIC50 | 68 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 5445-5448 [PMID:15454242] |
ChEMBL | Inhibition of human COX2 expressed in african green monkey COS cells assessed as inhibition of arachidonic acid-stimulated PGE2 production treated 1 hr before arachidonic acid challenge by enzyme immunoassay | B | 7.17 | pIC50 | 68 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 4504-4508 [PMID:19520573] |
ChEMBL | Inhibition of human recombinant COX2 by EIA | B | 7.19 | pIC50 | 65 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 5245-5250 [PMID:20655211] |
ChEMBL | Inhibition of human COX2 by enzyme immunoassay | B | 7.19 | pIC50 | 65 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 4544-4549 [PMID:20576432] |
ChEMBL | Inhibition of human COX2 expressed in baculovirus-infected SF9 cells assessed as inhibition of arachidonic acid-stimulated PGE2 production treated 1 hr before arachidonic acid challenge by enzyme immunoassay | B | 7.2 | pIC50 | 63 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 4504-4508 [PMID:19520573] |
ChEMBL | Inhibition of human COX2 by fluorescence based assay | B | 7.22 | pIC50 | 60 | nM | IC50 | Medchemcomm (2017) 8: 492-500 [PMID:30108767] |
ChEMBL | Inhibition of COX2 | B | 7.22 | pIC50 | 60 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 5634-5637 [PMID:17822894] |
ChEMBL | Inhibition of human recombinant COX2 by enzymatic fluorescence assay | B | 7.22 | pIC50 | 60 | nM | IC50 | Bioorg Med Chem (2012) 20: 3410-3421 [PMID:22560838] |
ChEMBL | Competitive inhibition of human recombinant COX2 by enzyme immunoassay | B | 7.22 | pIC50 | 60 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 2235-2238 [PMID:22341941] |
ChEMBL | Inhibition of COX-2 (unknown origin) by ELISA | B | 7.24 | pIC50 | 57 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 317-324 [PMID:24295787] |
ChEMBL | Inhibition of COX2 (unknown origin) | B | 7.24 | pIC50 | 57 | nM | IC50 | Med Chem Res (2013) 22: 1529-1537 |
ChEMBL | Inhibition of COX2 (unknown origin) expressed in HEK293 TRex cells assessed as reduction in PGE2 production using arachidonic acid as substrate preincubated for 60 mins followed by substrate addition for 1 hr in presence of 10% FBS by RapidFire High-Throughput Mass Spectrometry | B | 7.24 | pIC50 | 57 | nM | IC50 | J Med Chem (2021) 64: 11570-11596 [PMID:34279934] |
ChEMBL | Inhibitory concentration against Prostaglandin G/H synthase 2 | B | 7.25 | pIC50 | 56.7 | nM | IC50 | J Med Chem (2001) 44: 2921-2927 [PMID:11520200] |
ChEMBL | In vitro inhibitory concentration of compound required to inhibit Prostaglandin G/H synthase 2 enzyme was determined | B | 7.25 | pIC50 | 56.7 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 2753-2756 [PMID:12217369] |
ChEMBL | Inhibition of human recombinant COX-2 assessed as production of PGE2 using arachidonic acid as a substrate preincubated for 60 mins followed by substrate addition and measured after 2 mins by ELISA analysis | B | 7.25 | pIC50 | 56 | nM | IC50 | Bioorg Med Chem (2021) 46: 116344-116344 [PMID:34438337] |
ChEMBL | Inhibition of recombinant human COX-2 by enzyme immunoassay | B | 7.26 | pIC50 | 55 | nM | IC50 | RSC Med Chem (2022) 13: 471-496 [PMID:35685617] |
ChEMBL | Inhibition of COX-2 in human HNSCC 1483 cells using [14C] arachidonic acid as substrate preincubated for 30 mins before substrate addition measured after 30 mins | B | 7.27 | pIC50 | 54 | nM | IC50 | J Med Chem (2012) 55: 2287-2300 [PMID:22263894] |
ChEMBL | Compound was tested for the inhibition of recombinant human Prostaglandin G/H synthase 2 (COX-2) | B | 7.27 | pIC50 | 54 | nM | IC50 | J Med Chem (2003) 46: 5484-5504 [PMID:14640557] |
ChEMBL | Inhibition of human recombinant COX2 by ELISA | B | 7.28 | pIC50 | 52 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 1947-1951 [PMID:25866240] |
ChEMBL | Inhibitory concentration against Prostaglandin G/H synthase 2 | B | 7.29 | pIC50 | 50.7 | nM | IC50 | J Med Chem (2001) 44: 3039-3042 [PMID:11520213] |
ChEMBL | Inhibition of human recombinant COX2 by colorimetric analysis | B | 7.3 | pIC50 | 50 | nM | IC50 | Eur J Med Chem (2020) 200: 112439-112439 [PMID:32485532] |
ChEMBL | Inhibition of human recombinant COX2 pre-treated for 1 hr before 10-acetyl-3,7-dihydroxyphenoxazin substrate addition in absence of porcine liver esterase by fluorescence assay | B | 7.3 | pIC50 | 50 | nM | IC50 | ACS Med Chem Lett (2014) 5: 983-988 [PMID:25221653] |
ChEMBL | Inhibition of human recombinant COX2 catalytic activity using arachidonic acid as substrate pre-incubated for 10 mins followed by substrate addition and measured after 2 mins by ELISA method | B | 7.3 | pIC50 | 50 | nM | IC50 | Eur J Med Chem (2019) 167: 562-582 [PMID:30818268] |
ChEMBL | Inhibition of recombinant human COX2 assessed as reduction in PGF2alpha production using arachidonic acid as substrate by colorimetric method | B | 7.3 | pIC50 | 50 | nM | IC50 | Eur J Med Chem (2018) 144: 635-650 [PMID:29289887] |
ChEMBL | Inhibition of human recombinant COX2 assessed as reduction in PGH2 formation by measuring PGF2alpha by colorimetric assay | B | 7.3 | pIC50 | 50 | nM | IC50 | Bioorg Med Chem (2017) 25: 5637-5651 [PMID:28916158] |
ChEMBL | Inhibition of human recombinant COX-2 by EIA method | B | 7.31 | pIC50 | 49 | nM | IC50 | Eur J Med Chem (2019) 183: 111693-111693 [PMID:31539778] |
ChEMBL | Inhibition of human recombinant COX-2 | B | 7.31 | pIC50 | 49 | nM | IC50 | RSC Med Chem (2022) 13: 471-496 [PMID:35685617] |
ChEMBL | Inhibition of human COX-2 | B | 7.32 | pIC50 | 48 | nM | IC50 | Eur J Med Chem (2020) 200: 112438-112438 [PMID:32485533] |
ChEMBL | Inhibition of human recombinant COX2 using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition and measured after 2 mins by EIA | B | 7.35 | pIC50 | 45 | nM | IC50 | Bioorg Med Chem (2020) 28: 115403-115403 [PMID:32127262] |
ChEMBL | Inhibition of COX-2 (unknown origin) using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition measured after 2 mins by ELISA method | B | 7.35 | pIC50 | 45 | nM | IC50 | Eur J Med Chem (2023) 250: 115180-115180 [PMID:36796297] |
ChEMBL | Inhibition of human recombinant COX-2 using arachidonic acid as substrate preincubated with enzyme for 5 mins followed by substrate addition by colorimetric analysis | B | 7.35 | pIC50 | 45 | nM | IC50 | Eur J Med Chem (2021) 219: 113457-113457 [PMID:33892270] |
ChEMBL | Inhibition of human recombinant COX2 expressed in insect cells using arachidonic acid as substrate incubated for 1 min prior to substrate addition measured for 25 secs by TMPD-based chromogenic assay | B | 7.38 | pIC50 | 42 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 6745-6749 [PMID:23010270] |
ChEMBL | Inhibition of human recombinant COX-2 using arachidonic acid as substrate preincubated for 15 mins followed by substrate addition and measured after 2 mins by fluorescence based analysis | B | 7.39 | pIC50 | 40.95 | nM | IC50 | J Nat Prod (2023) 86: 2592-2619 [PMID:37856864] |
ChEMBL | Inhibition of COX2 (unknown origin) | B | 7.4 | pIC50 | 40 | nM | IC50 | J Med Chem (2021) 64: 17656-17689 [PMID:34905377] |
ChEMBL | Inhibition of human recombinant COX-2 expressed in insect cell system using arachidonic acid as substrate assessed as reduction of PGG2 to PGH2 incubated for 1 min prior to substrate addition measured after 25 secs by chromogenic assay | B | 7.4 | pIC50 | 40 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 2251-2255 [PMID:24745964] |
ChEMBL | Inhibition of human recombinant COX2 using arachidonic acid as substrate incubated for 10 mins prior to substrate addition measured after 2 mins by spectrophotometry | B | 7.4 | pIC50 | 40 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 77-82 [PMID:24332492] |
ChEMBL | Inhibition of human recombinant COX-2 assessed as decrease in prostaglandin production using arachidonic acid as substrate incubated with enzyme for 10 mins prior to substrate challenge by enzyme immunoassay | B | 7.4 | pIC50 | 40 | nM | IC50 | Eur J Med Chem (2014) 77: 185-192 [PMID:24631898] |
ChEMBL | Inhibition of COX2 (unknown origin) by solid phase ELISA method | B | 7.4 | pIC50 | 40 | nM | IC50 | Bioorg Med Chem (2014) 22: 4109-4118 [PMID:24934992] |
ChEMBL | Inhibition of human recombinant COX-2 assessed as PGF2 alpha formation using arachidonic acid as substrate pretreated with compound for 20 mins prior to substrate addition by spectrophotometric analysis | B | 7.4 | pIC50 | 40 | nM | IC50 | Eur J Med Chem (2015) 97: 104-123 [PMID:25956953] |
ChEMBL | Inhibition of COX2 | B | 7.4 | pIC50 | 40 | nM | IC50 | J Med Chem (2012) 55: 2287-2300 [PMID:22263894] |
ChEMBL | Inhibition of COX2 (unknown origin) | B | 7.4 | pIC50 | 40 | nM | IC50 | Medchemcomm (2015) 6: 2081-2123 |
ChEMBL | Inhibition of COX-2 (unknown origin) | B | 7.4 | pIC50 | 40 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 1516-1520 [PMID:26898334] |
ChEMBL | Inhibition of recombinant human COX-2 preincubated for 5 mins followed by addition of arachidonic acid as substrate measured after 2 mins by fluorescence analysis | B | 7.4 | pIC50 | 40 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 1516-1520 [PMID:26898334] |
ChEMBL | Inhibition of human recombinant COX2 assessed as reduction in PGH2-derived PGF2alpha using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition measured after 2 mins by enzyme immunoassay | B | 7.4 | pIC50 | 40 | nM | IC50 | J Med Chem (2016) 59: 3920-3934 [PMID:27019010] |
ChEMBL | Inhibition of human recombinant COX2 by fluorescence assay | B | 7.4 | pIC50 | 40 | nM | IC50 | Bioorg Med Chem (2012) 20: 2221-2226 [PMID:22386983] |
ChEMBL | Inhibition of human COX2 | B | 7.4 | pIC50 | 40 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 993-996 [PMID:21215625] |
ChEMBL | Inhibition of human COX2 pre-incubated for 10 mins before arachidonic acid addition and measured after 2 mins by EIA method | B | 7.4 | pIC50 | 40 | nM | IC50 | J Med Chem (2018) 61: 7929-7941 [PMID:30095904] |
ChEMBL | Inhibition of recombinant human COX-2 expressed in Baculovirus infected sf9 cells using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition measured after 10 mins by ELISA | B | 7.4 | pIC50 | 40 | nM | IC50 | Eur J Med Chem (2019) 162: 1-17 [PMID:30396033] |
ChEMBL | Inhibition of recombinant human COX-2 assessed as reduction in prostaglandin production preincubated for 10 mins followed by arachidonic acid addition and measured after 2 mins by EIA method | B | 7.4 | pIC50 | 40 | nM | IC50 | J Med Chem (2019) 62: 6363-6376 [PMID:31244108] |
ChEMBL | Inhibition of human COX2 using arachidonic acid as substrate incubated for 10 mins followed by substrate addition and measured after 2 mins by EIA assay | B | 7.4 | pIC50 | 40 | nM | IC50 | Bioorg Med Chem (2020) 28: 115246-115246 [PMID:31843462] |
ChEMBL | In vitro inhibitory concentration required to block human recombinant prostaglandin G/H synthase 2 (COX-2) | B | 7.4 | pIC50 | 40 | nM | IC50 | J Med Chem (1997) 40: 1347-1365 [PMID:9135032] |
ChEMBL | Inhibition of human COX-2 using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition and measured after 2 mins by EIA | B | 7.4 | pIC50 | 40 | nM | IC50 | J Med Chem (2021) 64: 9550-9566 [PMID:34137625] |
ChEMBL | In vitro inhibitory activity against human Prostaglandin G/H synthase 2 | B | 7.4 | pIC50 | 40 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 1171-1174 [PMID:10328307] |
ChEMBL | Inhibition of human COX2 using arachidonic acid as substrate assessed as PGE2 formation incubated for 10 mins prior to substrate addition measured after 10 mins by ELISA | B | 7.4 | pIC50 | 40 | nM | IC50 | Eur J Med Chem (2014) 76: 494-505 [PMID:24602792] |
ChEMBL | Inhibitory concentration against human prostaglandin G/H synthase 2 at 25 degrees. | B | 7.4 | pIC50 | 40 | nM | IC50 | Bioorg Med Chem Lett (2002) 12: 267-270 [PMID:11814774] |
ChEMBL | In Vitro activity of compound against human recombinant Prostaglandin G/H synthase 2 | B | 7.4 | pIC50 | 40 | nM | IC50 | J Med Chem (2000) 43: 775-777 [PMID:10715145] |
ChEMBL | In Vitro activity of compound against human recombinant Prostaglandin G/H synthase 2 | B | 7.4 | pIC50 | 40 | nM | IC50 | J Med Chem (2000) 43: 775-777 [PMID:10715145] |
ChEMBL | Inhibition of COX-2 (unknown origin) | B | 7.4 | pIC50 | 40 | nM | IC50 | Eur J Med Chem (2023) 256: 115443-115443 [PMID:37182334] |
ChEMBL | Inhibition of recombinant human COX-2 | B | 7.4 | pIC50 | 40 | nM | IC50 | Eur J Med Chem (2023) 256: 115443-115443 [PMID:37182334] |
ChEMBL | Inhibition of human Prostaglandin G/H synthase 2 | B | 7.4 | pIC50 | 39.81 | nM | IC50 | J Med Chem (2001) 44: 3223-3230 [PMID:11563921] |
ChEMBL | Inhibitory activity against human Prostaglandin G/H synthase 2 expressed in sf-9 cells infected with baculovirus | B | 7.44 | pIC50 | 36 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 499-504 [PMID:14698190] |
ChEMBL | In vitro inhibitory activity against recombinant human Prostaglandin G/H synthase 2 | B | 7.44 | pIC50 | 36 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 1639-1643 [PMID:12729631] |
ChEMBL | Inhibition of COX2 expressed in CHO cells assessed as inhibition of arachidonic acid-stimulated PGE2 production by enzyme immunoassay | F | 7.44 | pIC50 | 36 | nM | IC50 | J Med Chem (2004) 47: 6195-6206 [PMID:15566290] |
ChEMBL | In vitro inhibitory activity against human recombinant prostaglandin G/H synthase 2 expressed in sf-9 cells infected with baculovirus | B | 7.44 | pIC50 | 36 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 1683-1688 [PMID:15026050] |
ChEMBL | Inhibition of human recombinant COX-2 assessed as reduction in PGF2alpha formation using arachidonic acid as substrate preincubated with enzyme for 10 mins followed by substrate addition for 30 secs and measured after 1 hr by microplate reader based enzyme immunoassay | B | 7.45 | pIC50 | 35.56 | nM | IC50 | Eur J Med Chem (2019) 171: 332-342 [PMID:30928706] |
ChEMBL | Inhibition of human recombinant COX2 by measuring PGE2 | B | 7.46 | pIC50 | 35 | nM | IC50 | Bioorg Med Chem (2007) 15: 6109-6118 [PMID:17604631] |
ChEMBL | Inhibition of human recombinant COX2 using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition measured after 2 mins by ADHP probe-based fluorescence assay | B | 7.52 | pIC50 | 30 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 1721-1726 [PMID:28284805] |
ChEMBL | Inhibition of COX2 by fluorescence assay | B | 7.52 | pIC50 | 30 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 3567-3570 [PMID:22516282] |
ChEMBL | Inhibition of human recombinant COX-2 by fluorescence assay | B | 7.52 | pIC50 | 30 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1823-1826 [PMID:21316237] |
ChEMBL | Inhibition of human recombinant COX-2 assessed as reduction in peroxidase activity using arachidonic acid as substrate preincubated for 60 mins followed by substrate addition for 2 secs by ADPH based fluorometric analysis | B | 7.55 | pIC50 | 28 | nM | IC50 | J Med Chem (2021) 64: 11570-11596 [PMID:34279934] |
ChEMBL | Inhibition of human recombinant COX2 by fluorescence assay | B | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem (2013) 21: 4288-4295 [PMID:23706267] |
ChEMBL | Inhibition of recombinant human COX2 assessed as PGH2 formation preincubated for 10 mins followed by addition of arachidonic acid as substrate measured after 2 mins by ELISA | B | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 4757-4762 [PMID:27567369] |
ChEMBL | Inhibition of human recombinant COX2 using fluorometric substrate after 15 mins | B | 7.72 | pIC50 | 19 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 1986-1989 [PMID:25819096] |
ChEMBL | Inhibition of human recombinant COX-2 using arachidonic acid after 15 mins by fluorescence based assay | B | 7.72 | pIC50 | 19 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 4082-4084 [PMID:26316467] |
ChEMBL | Inhibition of human COX2 assessed as reduction in PGF2alpha production using arachidonic acid as substrate preincubated with enzyme for 10 mins followed by substrate addition by ELISA | B | 7.75 | pIC50 | 17.79 | nM | IC50 | Eur J Med Chem (2019) 171: 25-37 [PMID:30904755] |
ChEMBL | Inhibition of human recombinant COX2 pre-incubated for 15 mins followed by addition of heme and fluorometric substrate and further incubated for 15 mins in presence of arachidonic acid by fluorescence based assay | B | 7.8 | pIC50 | 16 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 2469-2472 [PMID:25980909] |
ChEMBL | Inhibition of COX2 (unknown origin) fluorescence based analysis | B | 7.82 | pIC50 | 15 | nM | IC50 | J Nat Prod (2023) 86: 2592-2619 [PMID:37856864] |
ChEMBL | Inhibition of COX-2 (unknown origin) using arachidonic acid as substrate and measured by fluorometric assay | B | 7.91 | pIC50 | 12.2 | nM | IC50 | Eur J Med Chem (2022) 241: 114597-114597 [PMID:35931005] |
ChEMBL | Inhibition of human COX2 assessed as reduction in PGF2alpha level using arachidonic acid as substrate preincubated for 10 mins followed by substrate addition by ELISA | B | 7.92 | pIC50 | 12 | nM | IC50 | Bioorg Med Chem (2018) 26: 141-151 [PMID:29191502] |
ChEMBL | Inhibition of human COX-2 using arachidonic acid as substrate incubated for 5 mins by fluorescence-based assay | B | 7.95 | pIC50 | 11.2 | nM | IC50 | Eur J Med Chem (2019) 180: 41-50 [PMID:31299586] |
ChEMBL | Inhibition of COX-2 (unknown origin) using arachidonic acid as substrate incubated for 1 min by absorbance based analysis | B | 7.99 | pIC50 | 10.25 | nM | IC50 | RSC Med Chem (2022) 13: 471-496 [PMID:35685617] |
ChEMBL | Inhibition of human recombinant COX-2 after 2 mins by fluorescence assay | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (2011) 54: 3037-3050 [PMID:21434686] |
ChEMBL | Inhibition of recombinant human COX-2 preincubated for 15 mins followed by fluorometric substrate/heme addition for 15 mins subsequently incubated with arachidonic acid for 2 mins by fluorescence analysis | B | 8.15 | pIC50 | 7 | nM | IC50 | J Med Chem (2017) 60: 4135-4146 [PMID:28475316] |
ChEMBL | Inhibitory concentration against COX-2; (valus obtained by Kato et al.) | B | 8.17 | pIC50 | 6.8 | nM | IC50 | J Med Chem (2005) 48: 6997-7004 [PMID:16250658] |
ChEMBL | Inhibition of human recombinant COX-2 using arachidonic acid as substrate by fluorescence assay | B | 8.22 | pIC50 | 6 | nM | IC50 | Eur J Med Chem (2021) 224: 113682-113682 [PMID:34245948] |
ChEMBL | Inhibitory concentration against COX-2 upon incubation for 15 minutes at 37 degree C | B | 8.22 | pIC50 | 6 | nM | IC50 | J Med Chem (2005) 48: 6997-7004 [PMID:16250658] |
ChEMBL | Inhibition of COX2 (unknown origin) using arachidonic acid as substrate pretreated for 10 mins followed by substrate addition measured after 2 mins by enzyme-immunoassay | B | 8.32 | pIC50 | 4.8 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 2377-2383 [PMID:28427813] |
ChEMBL | Inhibition of COX2 | B | 8.66 | pIC50 | 2.2 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 4483-4487 [PMID:16806914] |
ChEMBL | Inhibitory of human Prostaglandin G/H synthase 2 expressed in CHO cells. | B | 8.7 | pIC50 | 2 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 1195-1198 [PMID:12643942] |
ChEMBL | In vitro potency against human Prostaglandin G/H synthase 2 in transfected CHO cells. | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (1999) 42: 1274-1281 [PMID:10197970] |
ChEMBL | In vitro inhibitory potency against human COX-2 in stably transfected chinese hamster ovary (CHO) cells | B | 8.7 | pIC50 | 2 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 3181-3186 [PMID:10576684] |
ChEMBL | Inhibition of PGE-2 production in CHO cells expressing human COX-2. | B | 8.7 | pIC50 | 2 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 3187-3192 [PMID:10576685] |
GtoPdb | - | - | 8.7 | pIC50 | 2 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 1195-8 [PMID:12643942] |
ChEMBL | Inhibition of COX2 | B | 9.28 | pIC50 | 0.52 | nM | IC50 | Eur J Med Chem (2008) 43: 1297-1303 [PMID:17714833] |
ChEMBL | Inhibition of COX2 | B | 9.28 | pIC50 | 0.52 | nM | IC50 | Eur J Med Chem (2008) 43: 1297-1303 [PMID:17714833] |
Cyclooxygenase-2 in Dog (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4033] [UniProtKB: Q8SPQ9] | ||||||||
ChEMBL | In vitro inhibitory activity against canine prostaglandin G/H synthase 2. | B | 6.05 | pIC50 | 900 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 95-98 [PMID:14684306] |
Cyclooxygenase-2 in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3331] [UniProtKB: O62698] | ||||||||
ChEMBL | Inhibition of Bos taurus (bovine) COX-2 by Chemoiluminescence assay | B | 7.22 | pIC50 | 60 | nM | IC50 | Med Chem Res (2010) 19: 782-793 |
ChEMBL | In vitro inhibitory activity against prostaglandin G/H synthase 2 (COX-2) | B | 7.24 | pIC50 | 57 | nM | IC50 | J Med Chem (2003) 46: 4872-4882 [PMID:14584938] |
Cyclooxygenase-2 in Sheep (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4102] [UniProtKB: P79208] | ||||||||
ChEMBL | Inhibitory concentration against Prostaglandin G/H synthase 2 from sheep placenta at 100 uM | B | 5.69 | pIC50 | 2050 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 1793-1797 [PMID:15780608] |
ChEMBL | Inhibition of ovine COX2 by enzyme immuno assay | B | 5.77 | pIC50 | 1710 | nM | IC50 | Bioorg Med Chem (2008) 16: 3907-3916 [PMID:18272371] |
ChEMBL | Inhibition of Ovine COX-2 assessed as decrease in prostaglandin production using arachidonic acid as substrate pretreated for 15 mins followed by substrate addition and measured after 2 mins by enzyme immunoassay | B | 5.81 | pIC50 | 1540 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 2893-2899 [PMID:27158139] |
ChEMBL | Inhibition of ovine COX-2 assessed as reduction in PGF2-alpha formation using arachidonic acid as substrate by enzyme immunoassay | B | 5.81 | pIC50 | 1540 | nM | IC50 | Eur J Med Chem (2016) 118: 250-258 [PMID:27131067] |
ChEMBL | Inhibition of ovine COX-2 assessed as appearance of oxidized TMPD level by EIA method | B | 5.81 | pIC50 | 1540 | nM | IC50 | Eur J Med Chem (2016) 123: 803-813 [PMID:27541263] |
ChEMBL | Inhibition of ovine COX-2 | B | 5.95 | pIC50 | 1110 | nM | IC50 | RSC Med Chem (2022) 13: 1150-1196 [PMID:36325400] |
ChEMBL | Inhibition of ovine COX-2 colorimetric enzyme immunoassay | B | 6.05 | pIC50 | 890 | nM | IC50 | RSC Med Chem (2022) 13: 471-496 [PMID:35685617] |
ChEMBL | Inhibition of ovine COX2 | B | 6.18 | pIC50 | 660 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 3378-3381 [PMID:28610982] |
ChEMBL | Inhibition of ovine COX-2 using arachidonic acid after 5 mins by colorimetric method | B | 6.25 | pIC50 | 560 | nM | IC50 | Bioorg Med Chem (2015) 23: 6807-6814 [PMID:26455657] |
ChEMBL | Inhibition of ovine COX2 by colorimetric assay | B | 6.27 | pIC50 | 540 | nM | IC50 | Eur J Med Chem (2019) 162: 435-447 [PMID:30469039] |
ChEMBL | Inhibition of ovine COX2 | B | 6.36 | pIC50 | 440 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 4440-4443 [PMID:16814546] |
ChEMBL | Inhibition of ovine COX2 assessed as PGE2 formation preincubated for 10 mins by ELISA | B | 6.44 | pIC50 | 360 | nM | IC50 | Eur J Med Chem (2011) 46: 5763-5768 [PMID:22019186] |
ChEMBL | Inhibition of ovine COX2 assessed as reduction in PGF2alpha production using arachidonic acid as substrate preincubated with enzyme for 5 mins followed by substrate addition and measured after 2 mins by colorimetric analysis | B | 6.48 | pIC50 | 330 | nM | IC50 | Eur J Med Chem (2016) 121: 410-421 [PMID:27318118] |
ChEMBL | Inhibition of ovine COX2 assessed as PGF2alpha production from PGH2 after 5 mins by enzyme immunoassay | B | 6.52 | pIC50 | 300 | nM | IC50 | Bioorg Med Chem (2011) 19: 3416-3424 [PMID:21570309] |
ChEMBL | Inhibition of ovine COX2 using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition by ELISA | B | 6.52 | pIC50 | 300 | nM | IC50 | Bioorg Med Chem (2016) 24: 3818-3828 [PMID:27344214] |
ChEMBL | Inhibition of ovine COX2 assessed as reduction in PGH2-dervied PGF2alpha production preincubated for 5 mins followed by addition of arachidonic acid as substrate measured after 2 mins by enzyme immunoassay | B | 6.52 | pIC50 | 300 | nM | IC50 | Eur J Med Chem (2016) 115: 121-131 [PMID:26999325] |
ChEMBL | Inhibition of ovine COX-2 using arachidonic acid as substrate assessed as production of PGH2-alpha preincubated for 5 mins followed by addition of substrate measured after 2 mins by EIA | B | 6.52 | pIC50 | 300 | nM | IC50 | Bioorg Med Chem (2016) 24: 2032-2042 [PMID:27025563] |
ChEMBL | Inhibition of ovine COX2 | B | 6.52 | pIC50 | 300 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 5324-5329 [PMID:25444084] |
ChEMBL | Inhibition of ovine COX2 after 5 mins by enzyme immunoassay | B | 6.52 | pIC50 | 300 | nM | IC50 | Eur J Med Chem (2011) 46: 1648-1655 [PMID:21388719] |
ChEMBL | Inhibition of ovine COX2 assessed as reduction in PGH2-dervied PGF2alpha production using arachidonic acid substrate by enzyme immunoassay | B | 6.55 | pIC50 | 280 | nM | IC50 | Eur J Med Chem (2014) 87: 868-880 [PMID:24576797] |
ChEMBL | Inhibition of ovine COX2 by peroxidase activity-based colorimetric assay | B | 6.55 | pIC50 | 280 | nM | IC50 | Eur J Med Chem (2014) 74: 606-618 [PMID:24531199] |
ChEMBL | Inhibition of ovine COX2 by enzyme immuno assay | B | 6.55 | pIC50 | 280 | nM | IC50 | Bioorg Med Chem (2012) 20: 3306-3316 [PMID:22516672] |
ChEMBL | Inhibition of ovine COX2 assessed as reduction in PGH2 production using arachidonic acid substrate by enzyme immunoassay | B | 6.55 | pIC50 | 280 | nM | IC50 | Eur J Med Chem (2014) 86: 122-132 [PMID:25147154] |
ChEMBL | Inhibition of ovine COX2-mediated prostaglandin alpha production by enzyme immuno assay | B | 6.59 | pIC50 | 260 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 2601-2605 [PMID:23528298] |
ChEMBL | Inhibition of ovine COX2 assessed as inhibition of PGF2alpha production from PGH2 preincubated for 5 mins before arachidonic acid addition measured after 2 mins by enzyme immunoassay | B | 6.59 | pIC50 | 260 | nM | IC50 | Eur J Med Chem (2015) 92: 115-123 [PMID:25549551] |
ChEMBL | Inhibition of ovine COX2 using arachidonic acid as substrate assessed as conversion of PGH2 to PGF2alpha after 10 mins by EIA | B | 6.66 | pIC50 | 220 | nM | IC50 | Bioorg Med Chem (2014) 22: 2080-2089 [PMID:24631365] |
ChEMBL | Inhibition of ovine COX2 using arachidonic acid as substrate incubated for 5 mins followed by substrate addition measured after 2 mins by enzyme immunoassay | B | 6.74 | pIC50 | 180 | nM | IC50 | Medchemcomm (2016) 7: 2309-2327 |
ChEMBL | Inhibition of ovine COX2 using arachidonic acid as substrate preincubated for 10 mins before substrate addition measured after 5 mins by EIA | B | 6.82 | pIC50 | 150 | nM | IC50 | Eur J Med Chem (2014) 80: 47-56 [PMID:24763362] |
ChEMBL | Inhibition of ovine COX2 using arachidonic acid as substrate assessed as production of PGF2alpha preincubated for 10 mins followed by substrate addition measured after 2 mins by EIA in presence of stannous chloride | B | 6.82 | pIC50 | 150 | nM | IC50 | Bioorg Med Chem (2013) 21: 4581-4590 [PMID:23769654] |
ChEMBL | Inhibition of ovine COX2 assessed as reduction in PGF2alpha formation incubated for 18 hrs by enzyme immunoassay | B | 6.82 | pIC50 | 150 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 4638-4642 [PMID:25219899] |
ChEMBL | Inhibition of ovine COX-2 assessed as inhibition of transformation of AA to PGH2 by EIA | B | 6.95 | pIC50 | 113 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 6922-6925 [PMID:19880317] |
ChEMBL | Inhibition of ovine COX2 using arachidonic acid as substrate incubated for 5 mins followed by substrate addition measured after 2 mins by colorimetric based ELISA | B | 6.96 | pIC50 | 110 | nM | IC50 | Eur J Med Chem (2018) 158: 134-143 [PMID:30216848] |
ChEMBL | Inhibition of sheep COX2 by spectrophotometry | B | 7 | pIC50 | 100 | nM | IC50 | J Med Chem (2010) 53: 6560-6571 [PMID:20804197] |
ChEMBL | Inhibition of ovine COX2 by ELISA | B | 7 | pIC50 | 100 | nM | IC50 | Bioorg Med Chem Lett (2020) 30: 127173-127173 [PMID:32278513] |
ChEMBL | Inhibition of ovine COX2 using arachidonic acid substrate by TMPD dye based colorimetry | B | 7 | pIC50 | 100 | nM | IC50 | Medchemcomm (2017) 8: 492-500 [PMID:30108767] |
ChEMBL | Inhibitory activity against ovine COX2 | B | 7.15 | pIC50 | 70 | nM | IC50 | J Med Chem (2006) 49: 1668-1683 [PMID:16509583] |
ChEMBL | In vitro inhibition of ovine prostaglandin G/H synthase 2 | B | 7.15 | pIC50 | 70 | nM | IC50 | J Med Chem (2004) 47: 6108-6111 [PMID:15537365] |
ChEMBL | Inhibition of ovine COX2 assessed as inhibition of PGF2a formation after 20 mins by Ellman's method | B | 7.15 | pIC50 | 70 | nM | IC50 | J Med Chem (2010) 53: 3707-3717 [PMID:20387815] |
ChEMBL | In vitro inhibitory concentration against ovine Cyclooxygenase-2 | B | 7.15 | pIC50 | 70 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 439-442 [PMID:15603969] |
ChEMBL | In vitro inhibitory concentration against ovine Prostaglandin G/H synthase 2 | B | 7.15 | pIC50 | 70 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 4911-4914 [PMID:15341950] |
ChEMBL | Inhibition of ovine COX2 by enzyme-immuno assay | B | 7.15 | pIC50 | 70 | nM | IC50 | Eur J Med Chem (2009) 44: 3798-3804 [PMID:19457595] |
ChEMBL | Inhibition of ovine Prostaglandin G/H synthase 2 | B | 7.15 | pIC50 | 70 | nM | IC50 | J Med Chem (2004) 47: 3972-3990 [PMID:15267236] |
ChEMBL | In vitro inhibitory concentration against ovine Cyclooxygenase-2 | B | 7.15 | pIC50 | 70 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 439-442 [PMID:15603969] |
ChEMBL | Inhibition of ovine COX2 by enzyme immuno assay | B | 7.15 | pIC50 | 70 | nM | IC50 | Bioorg Med Chem (2008) 16: 9694-9698 [PMID:18930406] |
ChEMBL | Inhibition of ovine COX2 by enzyme immuno assay | B | 7.15 | pIC50 | 70 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 6138-6141 [PMID:18945614] |
ChEMBL | Inhibition of ovine COX2 by enzyme immunoassay | B | 7.15 | pIC50 | 70 | nM | IC50 | Bioorg Med Chem (2008) 16: 3302-3308 [PMID:18096394] |
ChEMBL | Inhibition of ovine COX2 by enzyme immuno assay | B | 7.15 | pIC50 | 70 | nM | IC50 | Bioorg Med Chem (2008) 16: 1948-1956 [PMID:18023187] |
ChEMBL | Inhibition of ovine COX2 by enzyme immuno assay | B | 7.15 | pIC50 | 70 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 6074-6080 [PMID:21890358] |
ChEMBL | Inhibition of ovine COX2 by enzyme immuno assay | B | 7.15 | pIC50 | 70 | nM | IC50 | Bioorg Med Chem (2007) 15: 6796-6801 [PMID:17764958] |
ChEMBL | Inhibition of ovine COX2 by chemiluminescent assay | B | 7.22 | pIC50 | 60 | nM | IC50 | Bioorg Med Chem Lett (2009) 19: 3162-3165 [PMID:19447036] |
ChEMBL | Inhibition of ovine COX2 by chemiluminescence assay | B | 7.22 | pIC50 | 60 | nM | IC50 | Eur J Med Chem (2010) 45: 4013-4017 [PMID:20691338] |
ChEMBL | Inhibition of Ovis aries (sheep) COX2 using arachidonic acid as substrate using cyclic naphthalene hydrazide by chemiluminescence assay | B | 7.22 | pIC50 | 60 | nM | IC50 | Med Chem Res (2012) 21: 1869-1875 |
ChEMBL | Inhibition of Ovis aries (sheep) COX2 using arachidonic acid as substrate using cyclic naphthalene hydrazide by chemiluminescence assay | B | 7.22 | pIC50 | 60 | nM | IC50 | Med Chem Res (2012) 21: 1803-1810 |
ChEMBL | Inhibition of Ovis aries (sheep) cyclooxygenase-2 using arachidonic acid as substrate by chemiluminescent assay | B | 7.22 | pIC50 | 60 | nM | IC50 | Med Chem Res (2013) 22: 3881-3887 |
ChEMBL | Inhibition of ovine COX2 using arachidonic acid as substrate by chemiluminescence assay | B | 7.22 | pIC50 | 60 | nM | IC50 | Bioorg Med Chem (2014) 22: 865-873 [PMID:24361187] |
ChEMBL | Inhibition of ovine COX2 by enzyme chemiluminescent enzyme assay | B | 7.22 | pIC50 | 60 | nM | IC50 | Bioorg Med Chem (2010) 18: 1029-1033 [PMID:20061161] |
ChEMBL | Inhibition of ovine COX2 by chemiluminescent enzyme assay | B | 7.22 | pIC50 | 60 | nM | IC50 | Bioorg Med Chem (2009) 17: 5312-5317 [PMID:19560931] |
ChEMBL | Inhibition of ovine COX2 by chemiluminescence assay | B | 7.22 | pIC50 | 60 | nM | IC50 | Bioorg Med Chem (2009) 17: 5369-5373 [PMID:19596198] |
ChEMBL | Inhibition of ovine COX2 by chemiluminescent assay | B | 7.22 | pIC50 | 60 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 1336-1339 [PMID:18226898] |
ChEMBL | Inhibition of Ovine COX-2 by chemiluminescent enzyme method | B | 7.22 | pIC50 | 60 | nM | IC50 | Bioorg Med Chem (2021) 32: 115960-115960 [PMID:33477020] |
ChEMBL | Inhibition of Ovis aries (sheep) COX-2 assessed as decrease in PGF2a production from PGH2 upon reduction with stannous chloride using arachidonic acid as substrate pre-incubated with enzyme for 5 min prior to substrate addition by enzyme immunoassay | B | 7.24 | pIC50 | 57 | nM | IC50 | Med Chem Res (2013) 22: 2493-2504 |
ChEMBL | In vitro inhibitory activity against prostaglandin G/H synthase 2 from ovine | B | 7.24 | pIC50 | 57 | nM | IC50 | Bioorg Med Chem Lett (2004) 14: 1953-1956 [PMID:15050635] |
ChEMBL | In vitro inhibition against ovine Prostaglandin G/H synthase 2 | B | 7.25 | pIC50 | 56.7 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 2205-2209 [PMID:12798335] |
ChEMBL | Inhibition of ovine COX2 assessed as reduction in PGH2 production by enzyme immunoassay | B | 7.29 | pIC50 | 50.7 | nM | IC50 | Bioorg Med Chem (2018) 26: 4113-4126 [PMID:29980364] |
ChEMBL | Inhibition of ovine COX2 assessed as reduction in oxidized TMPD using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition and measured after 2 mins by colorimetric assay | B | 7.3 | pIC50 | 50 | nM | IC50 | Eur J Med Chem (2019) 171: 372-382 [PMID:30928709] |
ChEMBL | Inhibition of ovine COX2 assessed as PGF2alpha level by EIA | B | 7.3 | pIC50 | 50 | nM | IC50 | Bioorg Med Chem (2011) 19: 2074-2083 [PMID:21349729] |
ChEMBL | Inhibition of ovine COX -2 by colorimetric inhibitor screening assay kit method | B | 7.3 | pIC50 | 50 | nM | IC50 | Eur J Med Chem (2019) 167: 161-186 [PMID:30771604] |
ChEMBL | Inhibition of sheep COX-2 by Cayman colorimetric analysis | B | 7.4 | pIC50 | 40 | nM | IC50 | RSC Med Chem (2022) 13: 522-567 [PMID:35694689] |
ChEMBL | Inhibition of ovine COX2 peroxidase activity assessed as reduction of PGG2 to PGH2 by measuring oxidized TMPD level by colorimetric assay | B | 7.4 | pIC50 | 40 | nM | IC50 | Bioorg Med Chem (2014) 22: 2855-2866 [PMID:24751552] |
ChEMBL | Inhibition of ovine COX2 by enzyme immunoassay | B | 7.4 | pIC50 | 40 | nM | IC50 | Bioorg Med Chem (2016) 24: 5626-5632 [PMID:27658794] |
ChEMBL | Inhibition of ovine COX2 | B | 7.4 | pIC50 | 40 | nM | IC50 | Bioorg Med Chem (2008) 16: 276-283 [PMID:17937989] |
COX-2 /Cyclooxygenase-2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4321] [GtoPdb: 1376] [UniProtKB: Q05769] | ||||||||
ChEMBL | Inhibition of COX2-dependent PGE2 production in LPS-stimulated mouse J774 cells at 10 uM by RIA | B | 4.02 | pIC50 | 95000 | nM | IC50 | J Med Chem (2010) 53: 723-733 [PMID:19957931] |
ChEMBL | Inhibition of COX2-dependent PGE2 production in LPS-stimulated mouse J774 cells at 1 uM by RIA | B | 4.1 | pIC50 | 80000 | nM | IC50 | J Med Chem (2010) 53: 723-733 [PMID:19957931] |
ChEMBL | Inhibition of mouse COX2 | B | 4.6 | pIC50 | >25000 | nM | IC50 | Bioorg Med Chem (2007) 15: 1976-1982 [PMID:17258905] |
ChEMBL | Inhibition of COX-2 in mouse RAW264.7 cells assessed as decrease in LPS-induced PGE2 production | B | 6.92 | pIC50 | 120 | nM | IC50 | Eur J Med Chem (2013) 62: 222-231 [PMID:23353741] |
ChEMBL | Inhibition of COX2-dependent PGE2 production in LPS-stimulated mouse J774 cells by RIA | B | 7.1 | pIC50 | 79 | nM | IC50 | J Med Chem (2010) 53: 723-733 [PMID:19957931] |
ChEMBL | In vitro inhibitory activity against Prostaglandin G/H synthase 2 in murine J774 cells | B | 7.1 | pIC50 | 79 | nM | IC50 | J Med Chem (2005) 48: 3428-3432 [PMID:15857149] |
ChEMBL | Inhibition of COX2 in LPS-stimulated mouse J774 cells assessed as inhibition of PGE2 production and measured after 24 hrs by enzyme immuno-assay (EIA) | B | 7.21 | pIC50 | 61 | nM | IC50 | Eur J Med Chem (2022) 241: 114615-114615 [PMID:35932568] |
ChEMBL | Inhibition of COX-2-mediated PGE2 production in LPS-stimulated mouse J774 cells after 24 hrs by radioimmunoassay | B | 7.21 | pIC50 | 61 | nM | IC50 | J Med Chem (2011) 54: 7759-7771 [PMID:21992176] |
ChEMBL | Inhibition of COX2 in mouse J774 cells assessed as inhibition of LPS-induced PGE2 production by radioimmunoassay | B | 7.21 | pIC50 | 61 | nM | IC50 | Bioorg Med Chem (2013) 21: 3695-3701 [PMID:23680444] |
ChEMBL | Inhibition of COX2 in LPS-stimulated J774 cells assessed as inhibition of PGE2 levels by radioimmunoassay | B | 7.22 | pIC50 | 60 | nM | IC50 | J Med Chem (2007) 50: 5403-5411 [PMID:17915854] |
ChEMBL | Inhibition of COX2 in LPS-stimulated mouse J774 cells assessed as inhibition of PGE2 production after 15 mins by radioimmunoassay | B | 7.22 | pIC50 | 60 | nM | IC50 | Bioorg Med Chem (2008) 16: 8072-8081 [PMID:18752957] |
ChEMBL | Inhibitory activity against prostaglandin G/H synthase 2 (COX-2) | B | 7.4 | pIC50 | 39.81 | nM | IC50 | J Med Chem (2002) 45: 4816-4827 [PMID:12383007] |
ChEMBL | Inhibition of mouse purified COX2 after 20 mins | B | 7.52 | pIC50 | 30 | nM | IC50 | ACS Med Chem Lett (2011) 2: 160-164 [PMID:21318094] |
ChEMBL | Tested for inhibition against Prostaglandin G/H synthase 1 from mouse resident macrophages | B | 8.03 | pIC50 | 9.3 | nM | IC50 | J Med Chem (2000) 43: 4582-4593 [PMID:11101350] |
ChEMBL | Inhibition of COX-2 in mouse RAW264.7 cells assessed as decrease in LPS-induced PGE2 production treated prior to LPS challenge by enzyme immunoassay | B | 8.06 | pIC50 | 8.7 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 1958-1962 [PMID:24656662] |
ChEMBL | In vivo inhibition of COX2 in po dosed C57BL/6J mouse model of spontaneous GI-tract tumor Apc-min assessed as chemopreventive effect by measuring reduction in polyp area and relevant plasma exposures | F | 8.49 | pIC50 | 3.2 | nM | IC50 | J Med Chem (2021) 64: 11570-11596 [PMID:34279934] |
ChEMBL | In vivo inhibition of COX2 in po dosed C57BL/6J mouse model of spontaneous GI-tract tumor Apc-min assessed as chemopreventive effect by measuring reduction in polyp area and relevant ileum exposures | F | 8.49 | pIC50 | 3.2 | nM | IC50 | J Med Chem (2021) 64: 11570-11596 [PMID:34279934] |
ChEMBL | Inhibition of LPS-induced COX2 activity in C57BL/6J mouse peritoneal macrophages by RIA | B | 9.29 | pIC50 | 0.51 | nM | IC50 | J Nat Prod (2006) 69: 1591-1595 [PMID:17125227] |
COX-2 /Cyclooxygenase-2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2977] [GtoPdb: 1376] [UniProtKB: P35355] | ||||||||
ChEMBL | In vitro inhibitory concentration against rat Prostaglandin G/H synthase 2 | B | 5.96 | pIC50 | 1100 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 2687-2690 [PMID:11591502] |
ChEMBL | Inhibition of COX2 in rat abdominal macrophages assessed as PGE2 production pretreated for 30 mins followed by addition of 10 uM arachidonic acid as substrate for 20 mins by EIA | B | 6.85 | pIC50 | 140 | nM | IC50 | Eur J Med Chem (2016) 108: 89-103 [PMID:26638042] |
ChEMBL | Inhibition of COX-2 in rat peritoneal macrophages assessed as reduction in PGE2 production using radiolabelled-arachidonic acid as substrate pretreated for 30 mins followed by substrate addition measured after 30 mins | B | 7.15 | pIC50 | 71 | nM | IC50 | Bioorg Med Chem (2017) 25: 4887-4893 [PMID:28757100] |
Cytochrome c oxidase subunit 1 in Sheep (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6011] [UniProtKB: O78749] | ||||||||
ChEMBL | Inhibition of ovine COX1 assessed as reduction in PGF2alpha incubated for 2 mins using arachidonic acid as substrate by ELISA | B | 4.56 | pIC50 | 27250 | nM | IC50 | Eur J Med Chem (2019) 182: 111601-111601 [PMID:31445233] |
ChEMBL | Inhibition of sheep COX1 | B | 4.61 | pIC50 | 24300 | nM | IC50 | Bioorg Med Chem (2010) 18: 5855-5860 [PMID:20650641] |
ChEMBL | Inhibition of ovine COX1 preincubated for 5 mins followed by arachidonic acid addition and measured after 2 mins by colorimetric method | B | 5.19 | pIC50 | 6500 | nM | IC50 | Bioorg Med Chem (2019) 27: 3979-3997 [PMID:31401008] |
Cytochrome c oxidase subunit 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6174] [UniProtKB: P00403] | ||||||||
ChEMBL | Inhibition of human COX2 assessed as reduction in PGF2alpha production by ELISA | B | 6.27 | pIC50 | 540 | nM | IC50 | Eur J Med Chem (2017) 139: 936-946 [PMID:28881288] |
ChEMBL | Inhibition of recombinant human COX2 assessed as reduction in PGF2alpha incubated for 2 mins using arachidonic acid as substrate by ELISA | B | 6.53 | pIC50 | 293 | nM | IC50 | Eur J Med Chem (2019) 182: 111601-111601 [PMID:31445233] |
ChEMBL | Inhibition of recombinant human COX2 expressed in baculovirus infected Sf21 cells using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition and measured after 5 mins by UV-visible spectrophotometric method | B | 6.55 | pIC50 | 280 | nM | IC50 | Eur J Med Chem (2020) 186: 111863-111863 [PMID:31740050] |
Cytochrome c oxidase subunit 2 in Sheep (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1250404] [UniProtKB: O78750] | ||||||||
ChEMBL | Inhibition of ovine COX-2 by colorimetric inhibitor screening assay | B | 6.8 | pIC50 | 160 | nM | IC50 | Eur J Med Chem (2021) 221: 113493-113493 [PMID:34029774] |
ChEMBL | Inhibition of ovine COX-2 using arachidonic acid as substrate measured after 2 mins by colorimetric enzyme immune assay | B | 7.05 | pIC50 | 90 | nM | IC50 | Eur J Med Chem (2021) 221: 113493-113493 [PMID:34029774] |
ChEMBL | Inhibition of sheep COX2 | B | 7.22 | pIC50 | 60 | nM | IC50 | Bioorg Med Chem (2010) 18: 5855-5860 [PMID:20650641] |
ChEMBL | Inhibition of ovine COX-2 colorimetric enzyme immunoassay | B | 7.37 | pIC50 | 42.6 | nM | IC50 | Eur J Med Chem (2021) 221: 113493-113493 [PMID:34029774] |
CYP2D6/Cytochrome P450 2D6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL289] [GtoPdb: 1329] [UniProtKB: P10635] | ||||||||
ChEMBL | DRUGMATRIX: CYP450, 2D6 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) | B | 6 | pIC50 | 1000 | nM | IC50 | DrugMatrix in vitro pharmacology data |
Delta carbonic anhydrase in Thalassiosira weissflogii (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3097982] [UniProtKB: Q5U9J1] | ||||||||
ChEMBL | Inhibition of Thalassiosira weissflogii delta carbonic anhydrase preincubated for 15 mins by stopped flow CO2 hydration assay | B | 6.58 | pKi | 265 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 275-279 [PMID:24314394] |
D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728] | ||||||||
ChEMBL | DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390) | B | 4.85 | pKi | 13997 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Dopamine D1 radioligand binding (ligand: [3H] SCH-23390) | B | 4.55 | pIC50 | 27994 | nM | IC50 | DrugMatrix in vitro pharmacology data |
DAT/Dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959] | ||||||||
ChEMBL | DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) | B | 5.71 | pKi | 1931 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Dopamine Transporter radioligand binding (ligand: [125I] RTI-55) | B | 5.61 | pIC50 | 2431 | nM | IC50 | DrugMatrix in vitro pharmacology data |
epoxide hydrolase 2/Epoxide hydratase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2409] [GtoPdb: 2970] [UniProtKB: P34913] | ||||||||
ChEMBL | Inhibition of human recombinant soluble epoxide hydrolase after 10 mins by fluorescent-based assay | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2011) 54: 3037-3050 [PMID:21434686] |
histone deacetylase 1/Histone deacetylase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL325] [GtoPdb: 2658] [UniProtKB: Q13547] | ||||||||
ChEMBL | Inhibition of full length recombinant human C-terminal FLAG/His-tagged HDAC1 expressed in baculovirus infected sf9 cells using Boc-Lys-(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence assay | B | 5.93 | pIC50 | 1185 | nM | IC50 | Bioorg Med Chem (2018) 26: 1418-1425 [PMID:29500130] |
histone deacetylase 6/Histone deacetylase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7] | ||||||||
ChEMBL | Inhibition of full length recombinant human N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 cells using Boc-Lys-(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence assay | B | 6.19 | pIC50 | 643 | nM | IC50 | Bioorg Med Chem (2018) 26: 1418-1425 [PMID:29500130] |
mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539] | ||||||||
ChEMBL | Inhibitory concentration against p38 alpha MAP kinase calculated by CoMFA model; FlexX score=-12.4 kcal/mol | B | 6.09 | pIC50 | 810 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 3506-3509 [PMID:15990304] |
NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975] | ||||||||
ChEMBL | DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) | B | 5.14 | pKi | 7247 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Norepinephrine Transporter radioligand binding (ligand: [125I] RTI-55) | B | 5.14 | pIC50 | 7308 | nM | IC50 | DrugMatrix in vitro pharmacology data |
phosphodiesterase 5A/Phosphodiesterase 5A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1827] [GtoPdb: 1304] [UniProtKB: O76074] | ||||||||
ChEMBL | Inhibition of recombinant 6His-tagged PDE5A1 catalytic domain (unknown origin) expressed in Escherichia coli using TAMRA-cGMP or FAM-cAMP as substrate incubated for 1.5 hrs by IMAP-FP assay | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2021) 64: 4462-4477 [PMID:33793216] |
ChEMBL | Inhibition of recombinant full length GST-tagged PDE5A1 (unknown origin) expressed in baculovirus infected Sf9 insect cells using TAMRA-cGMP as substrate incubated for 1.5 hrs by IMAP-FP assay | B | 4.43 | pIC50 | 37000 | nM | IC50 | J Med Chem (2021) 64: 4462-4477 [PMID:33793216] |
ChEMBL | Fluorescence Polarization Assay: PDE activity was measured using the IMAP fluorescence polarization assay (Molecular Devices) in which binding of hydrolyzed cyclic nucleotide substrate to immobilized metal coordination complexes increases fluorescence polarization (FP). Tetramethylrhodamine (TAMRA)-cGMP and fluorescein-cAMP were used as substrates, each at final concentration of 50 nmol/L. The PDE assay was done according to the manufacturer's specifications using either whole cell lysates or recombinant enzymes. FP was measured at excitation, emission wavelengths of either 530,590 nm for TAMRA-cGMP or 485,530 nm for fluorescein-cAMP using a Synergy4 (Biotek) microplate reader. | B | 4.44 | pIC50 | 36000 | nM | IC50 | US-9388139-B2. Derivatives of celeboxib, use thereof and preparation thereof (2016) |
PROBABLE TRANSMEMBRANE CARBONIC ANHYDRASE (CARBONATE DEHYDRATASE) (CARBONIC DEHYDRATASE) in Mycobacterium tuberculosis (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5767] [UniProtKB: P96878] | ||||||||
ChEMBL | Inhibition of Mycobacterium tuberculosis recombinant carbonic anhydrase Rv3273 pre-incubated for 15 mins by stopped-flow CO2 hydration method | B | 5.11 | pKi | 7760 | nM | Ki | J Med Chem (2012) 55: 9619-9629 [PMID:23067387] |
Progesterone receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1909044] [UniProtKB: Q690N0] | ||||||||
ChEMBL | DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020) | B | 5.63 | pKi | 2362 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Progesterone radioligand binding (ligand: [3H] R-5020) | B | 4.74 | pIC50 | 18109 | nM | IC50 | DrugMatrix in vitro pharmacology data |
mPGES1/Prostaglandin E synthase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5658] [GtoPdb: 1377] [UniProtKB: O14684] | ||||||||
ChEMBL | Inhibition of mPGES1 (unknown origin) by enzymatic assay | B | 6.27 | pIC50 | 540 | nM | IC50 | J Med Chem (2016) 59: 194-205 [PMID:26653180] |
ChEMBL | Inhibition of mPGES-1 in human whole blood assessed as reduction in LPS-induced PGE2 production preincubated for 30 mins followed by LPS stimulation for 20 to 24 hrs by LC/MS/MS analysis | B | 6.27 | pIC50 | 540 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 4824-4828 [PMID:27554445] |
ChEMBL | Inhibition of human microsomal PGES1 expressed in 293E cells by LC/MS/MS analysis | B | 6.37 | pIC50 | 425 | nM | IC50 | J Med Chem (2016) 59: 194-205 [PMID:26653180] |
Quinolone resistance protein norA in S.aureus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5114] [UniProtKB: P0A0J7] | ||||||||
ChEMBL | Inhibition of norA-mediated EtBr efflux in Staphylococcus aureus SA1199B overexpressing norA and expressing A116E GrlA mutation by fluorometry | B | 4.4 | pIC50 | >40000 | nM | IC50 | J Med Chem (2012) 55: 3568-3572 [PMID:22432682] |
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645] | ||||||||
ChEMBL | DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) | B | 5.48 | pKi | 3334 | nM | Ki | DrugMatrix in vitro pharmacology data |
ChEMBL | DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine) | B | 5.2 | pIC50 | 6276 | nM | IC50 | DrugMatrix in vitro pharmacology data |
Uncharacterized protein Rv1284/MT1322 in Mycobacterium tuberculosis (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5631] [UniProtKB: P9WPJ7] | ||||||||
ChEMBL | Inhibition of Mycobacterium tuberculosis recombinant carbonic anhydrase 1 encoded by Rv1284 by stopped flow CO2 hydration assay | B | 4.99 | pKi | 10350 | nM | Ki | J Med Chem (2009) 52: 3116-3120 [PMID:19338333] |
ChEMBL | Inhibition of Mycobacterium tuberculosis recombinant carbonic anhydrase Rv1284 pre-incubated for 15 mins by stopped-flow CO2 hydration method | B | 4.99 | pKi | 10350 | nM | Ki | J Med Chem (2012) 55: 9619-9629 [PMID:23067387] |
TRPV1/Vanilloid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4794] [GtoPdb: 507] [UniProtKB: Q8NER1] | ||||||||
ChEMBL | Inhibition of TRPV1 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2023) 80: 129101-129101 [PMID:36481449] |
Voltage-dependent L-type calcium channel subunit alpha-1C in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2366456] [UniProtKB: O35505] | ||||||||
ChEMBL | Inhibition of Cav1.2 calcium current measured using whole Cell patch clamp in guinea pig ventricular myocytes | F | 4.97 | pIC50 | 10600 | nM | IC50 | IC50 data for the L-type calcium channel extracted from a set of literature articles |
ChEMBL data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]