saccharin [Ligand Id: 5432] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL310671 (Benzosulfinide, E954, E-954(I), Gluside, INS-954(I), INS NO.954(I), NSC-5349, Saccharin, Saccharinum) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 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 | 7.02 | pKi | 95.3 | nM | Ki | Bioorg Med Chem (2015) 23: 2303-2309 [PMID:25882523] |
| 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 | 7.39 | pKi | 40.3 | 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 | 7.39 | pKi | 40.3 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 710-714 [PMID:21208801] |
| 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 | 6.12 | pKi | 751 | nM | Ki | Bioorg Med Chem (2012) 20: 1403-1410 [PMID:22285172] |
| butyrylcholinesterase/Butyrylcholinesterase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1914] [GtoPdb: 2471] [UniProtKB: P06276] | ||||||||
| ChEMBL | Inhibition of BuChE (unknown origin) assessed as reduction in S-butyrylthiocholine chloride hydrolysis after 15 mins by Ellman method | B | 5.44 | pIC50 | 3600 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 626-630 [PMID:25537270] |
| 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 | 6.06 | pKi | 876 | 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 | 6.1 | pKi | 792 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 6649-6654 [PMID:19846301] |
| 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 | 6.98 | pKi | 104 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 710-714 [PMID:21208801] |
| 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 | 6.13 | pKi | 736 | nM | Ki | Bioorg Med Chem (2009) 17: 4503-4509 [PMID:19450983] |
| 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 | 4.9 | pKi | 12500 | nM | Ki | Bioorg Med Chem (2009) 17: 1158-1163 [PMID:19124253] |
| 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 | 6.03 | pKi | 933 | 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 recombinant human carbonic anhydrase 1 expressed in Escherichia coli L21-GOLD (DE3) incubated for 10 mins prior to testing by stopped-flow CO2 hydration assay | B | 4.7 | pKi | >20000 | nM | Ki | J Med Chem (2018) 61: 1176-1181 [PMID:29266943] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 1 by stopped flow CO2 hydration method | B | 4.73 | pKi | 18540 | nM | Ki | J Med Chem (2009) 52: 2226-2232 [PMID:19317447] |
| ChEMBL | Inhibition of human recombinant CA1 by stopped-flow CO2 hydrase assay | B | 4.73 | pKi | 18540 | nM | Ki | Bioorg Med Chem (2009) 17: 1158-1163 [PMID:19124253] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 1 by stopped flow CO2 hydration assay | B | 4.73 | pKi | 18540 | 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 | 4.73 | pKi | 18540 | nM | Ki | Bioorg Med Chem (2009) 17: 4503-4509 [PMID:19450983] |
| ChEMBL | Inhibition of human recombinant CA1 by stopped-flow CO2 assay | B | 4.73 | pKi | 18540 | nM | Ki | Bioorg Med Chem (2009) 17: 5054-5058 [PMID:19520577] |
| ChEMBL | Inhibition of wild type human recombinant carbonic anhydrase 1 expressed in Escherichia coli BL21 (DE3) after 15 mins by CO2 hydration method | B | 4.73 | pKi | 18540 | nM | Ki | Bioorg Med Chem (2010) 18: 5498-5503 [PMID:20624682] |
| ChEMBL | Inhibition of human recombinant CA1 by stopped-flow CO2 hydration assay | B | 4.73 | pKi | 18540 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 710-714 [PMID:21208801] |
| ChEMBL | Inhibition of human carbonic anhydrase 1 after 15 mins by CO2 hydrase assay at pH 7.5 | B | 4.73 | pKi | 18540 | nM | Ki | Bioorg Med Chem (2011) 19: 1847-1851 [PMID:21377369] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 1 at pH 7.5 by stopped flow CO2 hydration assay | B | 4.73 | pKi | 18540 | nM | Ki | Bioorg Med Chem (2011) 19: 5023-5030 [PMID:21757360] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 1 after 15 mins by stopped flow CO2 hydration assay | B | 4.73 | pKi | 18540 | nM | Ki | Bioorg Med Chem (2012) 20: 1403-1410 [PMID:22285172] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 1 preincubated for 15 mins by stopped-flow CO2 hydrase assay | B | 4.73 | pKi | 18540 | 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 | 4.73 | pKi | 18540 | nM | Ki | J Med Chem (2013) 56: 1761-1771 [PMID:23391336] |
| ChEMBL | Inhibition of human esterase activity of carbonic anhydrase 1 using 4-nitrophenylacetate as substrate after 3 mins by spectrophotometric analysis | B | 4.73 | pKi | 18540 | nM | Ki | Bioorg Med Chem (2013) 21: 1522-1525 [PMID:22974493] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 1 preincubated for 15 mins by CO2 hydration stopped-flow assay | B | 4.73 | pKi | 18540 | nM | Ki | Bioorg Med Chem (2013) 21: 1534-1538 [PMID:22883029] |
| ChEMBL | Inhibition of human carbonic anhydrase 1 by stopped-flow CO2 hydrase assay | B | 4.73 | pKi | 18540 | nM | Ki | Bioorg Med Chem (2014) 22: 1821-1831 [PMID:24560739] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 1 expressed in Escherichia coli by stopped flow CO2 hydration assay | B | 4.73 | pKi | 18540 | nM | Ki | J Med Chem (2014) 57: 3522-3531 [PMID:24689792] |
| ChEMBL | Inhibition of human carbonic anhydrase-1 by stopped-flow CO2 hydration assay | B | 4.73 | pKi | 18540 | 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 | 4.73 | pKi | 18540 | nM | Ki | Bioorg Med Chem (2014) 22: 4537-4543 [PMID:25129169] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 1 by stopped flow CO2 hydrase assay | B | 4.73 | pKi | 18540 | 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 | 4.73 | pKi | 18540 | nM | Ki | Bioorg Med Chem (2015) 23: 2303-2309 [PMID:25882523] |
| ChEMBL | Inhibition of human CA1 incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay | B | 4.73 | pKi | 18540 | 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 | 4.73 | pKi | 18540 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 401-405 [PMID:26691758] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 1 preincubated for 15 mins by stopped flow CO2 hydration assay | B | 4.73 | pKi | 18540 | nM | Ki | Bioorg Med Chem (2016) 24: 1095-1105 [PMID:26810710] |
| ChEMBL | Inhibition of human Carbonic anhydrase1 using CO2 as substrate preincubated for 15 mins by stopped-flow CO2 hydration assay | B | 4.73 | pKi | 18540 | 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 | 4.73 | pKi | 18540 | 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 | 4.73 | pKi | 18540 | nM | Ki | Bioorg Med Chem Lett (2017) 27: 490-495 [PMID:28025002] |
| ChEMBL | Inhibition of recombinant human carbonic anhydrase-1 assessed as reduction in CO2 hydration preincubated for 10 mins measured for 5 to 10 secs by stopped flow assay | B | 4.73 | pKi | 18540 | nM | Ki | Bioorg Med Chem (2017) 25: 3583-3589 [PMID:28416101] |
| ChEMBL | Inhibition of human recombinant CA1 by CO2 hydration stopped flow assay | B | 4.73 | pKi | 18540 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 836-841 [PMID:18042384] |
| ChEMBL | Inhibition of human carbonic anhydrase 1 preincubated for 15 mins by stopped flow CO2 hydration assay | B | 4.73 | pKi | 18540 | nM | Ki | J Med Chem (2016) 59: 6547-6552 [PMID:27305384] |
| carbonic anhydrase 2/Carbonic anhydrase II in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL205] [GtoPdb: 3092] [UniProtKB: P00918] | ||||||||
| 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 | 5.13 | pKi | 7470 | nM | Ki | Bioorg Med Chem (2012) 20: 2208-2213 [PMID:22386980] |
| ChEMBL | Inhibition of recombinant human carbonic anhydrase 2 expressed in Escherichia coli L21-GOLD (DE3) incubated for 10 mins prior to testing by stopped-flow CO2 hydration assay | B | 5.22 | pKi | 6000 | nM | Ki | J Med Chem (2018) 61: 1176-1181 [PMID:29266943] |
| ChEMBL | Binding affinity to carbonic anhydrase 2 (unknown origin) | B | 5.22 | pKi | 6000 | nM | Ki | ACS Med Chem Lett (2018) 9: 657-661 [PMID:30034596] |
| ChEMBL | Inhibition of human recombinant Carbonic anhydrase 2 compound preincubated for 15 mins by stopped flow CO2 hydrase assay method | B | 5.22 | pKi | 5959 | nM | Ki | Bioorg Med Chem (2014) 22: 4537-4543 [PMID:25129169] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 2 by stopped flow CO2 hydrase assay | B | 5.22 | pKi | 5959 | 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 | 5.22 | pKi | 5959 | nM | Ki | Bioorg Med Chem (2015) 23: 2303-2309 [PMID:25882523] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase-2 by stopped flow CO2 hydrase assay method | B | 5.22 | pKi | 5959 | nM | Ki | Bioorg Med Chem Lett (2015) 25: 3550-3555 [PMID:26174556] |
| ChEMBL | Inhibition of recombinant human carbonic anhydrase-2 by stopped flow CO2 hydrase assay | B | 5.22 | pKi | 5959 | 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 | 5.22 | pKi | 5959 | nM | Ki | Bioorg Med Chem (2016) 24: 1115-1120 [PMID:26850377] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 2 preincubated for 15 mins by stopped-flow CO2 hydrase assay | B | 5.22 | pKi | 5959 | nM | Ki | J Med Chem (2012) 55: 10742-10748 [PMID:23181552] |
| ChEMBL | Inhibition of human carbonic anhydrase 2 preincubated for 15 mins by CO2 hydrase stopped flow assay | B | 5.22 | pKi | 5959 | 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 | 5.22 | pKi | 5959 | 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 | 5.22 | pKi | 5959 | nM | Ki | Bioorg Med Chem Lett (2017) 27: 490-495 [PMID:28025002] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 2 by stopped flow CO2 hydration assay | B | 5.22 | pKi | 5959 | nM | Ki | J Med Chem (2013) 56: 1761-1771 [PMID:23391336] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 2 after 15 mins by CO2 hydration method | B | 5.22 | pKi | 5959 | nM | Ki | Bioorg Med Chem (2010) 18: 5498-5503 [PMID:20624682] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 2 preincubated for 15 mins by stopped flow CO2 hydration assay | B | 5.22 | pKi | 5959 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 275-279 [PMID:24314394] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 2 preincubated for 15 mins by CO2 hydration stopped-flow assay | B | 5.22 | pKi | 5959 | nM | Ki | Bioorg Med Chem (2013) 21: 1534-1538 [PMID:22883029] |
| ChEMBL | Inhibition of human wild type carbonic anhydrase 2 expressed in Escherichia coli after 15 mins preincubation by stopped flow CO2 hydration assay | B | 5.22 | pKi | 5959 | nM | Ki | Bioorg Med Chem (2012) 20: 2208-2213 [PMID:22386980] |
| ChEMBL | Inhibition of human carbonic anhydrase-2 by stopped-flow CO2 hydration assay | B | 5.22 | pKi | 5959 | nM | Ki | Bioorg Med Chem (2014) 22: 2939-2946 [PMID:24792813] |
| ChEMBL | Inhibition of human carbonic anhydrase 2 preincubated for 15 mins by stopped flow CO2 hydration assay | B | 5.23 | pKi | 5950 | nM | Ki | J Med Chem (2016) 59: 6547-6552 [PMID:27305384] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 2 by stopped flow CO2 hydration method | B | 5.23 | pKi | 5950 | nM | Ki | J Med Chem (2009) 52: 2226-2232 [PMID:19317447] |
| ChEMBL | Inhibition of human recombinant CA2 by stopped-flow CO2 hydrase assay | B | 5.23 | pKi | 5950 | nM | Ki | Bioorg Med Chem (2009) 17: 1158-1163 [PMID:19124253] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 2 by stopped flow CO2 hydration assay | B | 5.23 | pKi | 5950 | 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 | 5.23 | pKi | 5950 | nM | Ki | Bioorg Med Chem (2009) 17: 4503-4509 [PMID:19450983] |
| ChEMBL | Inhibition of human recombinant CA2 by stopped-flow CO2 assay | B | 5.23 | pKi | 5950 | nM | Ki | Bioorg Med Chem (2009) 17: 5054-5058 [PMID:19520577] |
| ChEMBL | Inhibition of human recombinant CA2 by stopped-flow hydration assay | B | 5.23 | pKi | 5950 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 6649-6654 [PMID:19846301] |
| ChEMBL | Inhibition of human recombinant CA2 by stopped-flow CO2 hydration assay | B | 5.23 | pKi | 5950 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 710-714 [PMID:21208801] |
| ChEMBL | Inhibition of human carbonic anhydrase 2 after 15 mins by CO2 hydrase assay at pH 7.5 | B | 5.23 | pKi | 5950 | nM | Ki | Bioorg Med Chem (2011) 19: 1847-1851 [PMID:21377369] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 2 at pH 7.5 by stopped flow CO2 hydration assay | B | 5.23 | pKi | 5950 | nM | Ki | Bioorg Med Chem (2011) 19: 5023-5030 [PMID:21757360] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 2 after 15 mins by stopped flow CO2 hydration assay | B | 5.23 | pKi | 5950 | nM | Ki | Bioorg Med Chem (2012) 20: 1403-1410 [PMID:22285172] |
| ChEMBL | Inhibition of human esterase activity of carbonic anhydrase 2 using 4-nitrophenylacetate as substrate after 3 mins by spectrophotometric analysis | B | 5.23 | pKi | 5950 | nM | Ki | Bioorg Med Chem (2013) 21: 1522-1525 [PMID:22974493] |
| ChEMBL | Inhibition of human carbonic anhydrase 2 by stopped-flow CO2 hydrase assay | B | 5.23 | pKi | 5950 | nM | Ki | Bioorg Med Chem (2014) 22: 1821-1831 [PMID:24560739] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 2 expressed in Escherichia coli by stopped flow CO2 hydration assay | B | 5.23 | pKi | 5950 | nM | Ki | J Med Chem (2014) 57: 3522-3531 [PMID:24689792] |
| ChEMBL | Inhibition of human CA2 incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay | B | 5.23 | pKi | 5950 | nM | Ki | Bioorg Med Chem Lett (2015) 25: 5485-5489 [PMID:26525863] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 2 preincubated for 15 mins by stopped flow CO2 hydration assay | B | 5.23 | pKi | 5950 | nM | Ki | Bioorg Med Chem (2016) 24: 1095-1105 [PMID:26810710] |
| ChEMBL | Inhibition of recombinant human carbonic anhydrase-2 assessed as reduction in CO2 hydration preincubated for 10 mins measured for 5 to 10 secs by stopped flow assay | B | 5.23 | pKi | 5950 | nM | Ki | Bioorg Med Chem (2017) 25: 3583-3589 [PMID:28416101] |
| ChEMBL | Inhibition of human recombinant CA2 by CO2 hydration stopped flow assay | B | 5.23 | pKi | 5950 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 836-841 [PMID:18042384] |
| 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 | 5.29 | pKi | 5180 | nM | Ki | Bioorg Med Chem (2012) 20: 2208-2213 [PMID:22386980] |
| carbonic anhydrase 4/Carbonic anhydrase IV in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3729] [GtoPdb: 2599] [UniProtKB: P22748] | ||||||||
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 4 expressed in Escherichia coli by stopped flow CO2 hydration assay | B | 5.1 | pKi | 7920 | nM | Ki | J Med Chem (2014) 57: 3522-3531 [PMID:24689792] |
| carbonic anhydrase 9/Carbonic anhydrase IX in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3594] [GtoPdb: 3055] [UniProtKB: Q16790] | ||||||||
| ChEMBL | Inhibition of human carbonic anhydrase 9 catalytic site preincubated for 15 mins by stopped flow CO2 hydration assay | B | 6.99 | pKi | 103 | nM | Ki | J Med Chem (2016) 59: 6547-6552 [PMID:27305384] |
| ChEMBL | Inhibition of human esterase activity of carbonic anhydrase 9 using 4-nitrophenylacetate as substrate after 3 mins by spectrophotometric analysis | B | 6.99 | pKi | 103 | nM | Ki | Bioorg Med Chem (2013) 21: 1522-1525 [PMID:22974493] |
| ChEMBL | Inhibition of human carbonic anhydrase 9 by stopped-flow CO2 hydrase assay | B | 6.99 | pKi | 103 | nM | Ki | Bioorg Med Chem (2014) 22: 1821-1831 [PMID:24560739] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 9 expressed in Escherichia coli by stopped flow CO2 hydration assay | B | 6.99 | pKi | 103 | nM | Ki | J Med Chem (2014) 57: 3522-3531 [PMID:24689792] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 9 preincubated for 15 mins by stopped flow CO2 hydration assay | B | 6.99 | pKi | 103 | nM | Ki | Bioorg Med Chem (2016) 24: 1095-1105 [PMID:26810710] |
| ChEMBL | Inhibition of recombinant human carbonic anhydrase-9 assessed as reduction in CO2 hydration preincubated for 10 mins measured for 5 to 10 secs by stopped flow assay | B | 6.99 | pKi | 103 | nM | Ki | Bioorg Med Chem (2017) 25: 3583-3589 [PMID:28416101] |
| ChEMBL | Inhibition of recombinant human carbonic anhydrase 9 incubated for 1 hr prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | B | 6.99 | pKi | 103 | nM | Ki | J Med Chem (2020) 63: 321-333 [PMID:31794211] |
| ChEMBL | Inhibition of human recombinant CA9 by CO2 hydration stopped flow assay | B | 6.99 | pKi | 103 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 836-841 [PMID:18042384] |
| ChEMBL | Inhibition of recombinant human carbonic anhydrase 9 expressed in Escherichia coli L21-GOLD (DE3) incubated for 10 mins prior to testing by stopped-flow CO2 hydration assay | B | 7 | pKi | 100 | nM | Ki | J Med Chem (2018) 61: 1176-1181 [PMID:29266943] |
| ChEMBL | Binding affinity to carbonic anhydrase 9 (unknown origin) expressed in Escherichia coli BL21 (DE3) | B | 7 | pKi | 100 | nM | Ki | ACS Med Chem Lett (2018) 9: 657-661 [PMID:30034596] |
| 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 expressed in Escherichia coli by stopped flow CO2 hydration assay | B | 5 | pKi | 10060 | nM | Ki | J Med Chem (2014) 57: 3522-3531 [PMID:24689792] |
| Carbonic anhydrase VB in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3969] [UniProtKB: Q9Y2D0] | ||||||||
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 5B expressed in Escherichia coli by stopped flow CO2 hydration assay | B | 5.14 | pKi | 7210 | nM | Ki | J Med Chem (2014) 57: 3522-3531 [PMID:24689792] |
| Carbonic anhydrase VI in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3025] [UniProtKB: P23280] | ||||||||
| ChEMBL | Inhibition of human recombinant CA6 by stopped-flow CO2 hydration assay | B | 6.03 | pKi | 935 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 710-714 [PMID:21208801] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 6 expressed in Escherichia coli by stopped flow CO2 hydration assay | B | 6.03 | pKi | 935 | nM | Ki | J Med Chem (2014) 57: 3522-3531 [PMID:24689792] |
| 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 expressed in Escherichia coli by stopped flow CO2 hydration assay | B | 8 | pKi | 10 | nM | Ki | J Med Chem (2014) 57: 3522-3531 [PMID:24689792] |
| ChEMBL | Inhibition of human carbonic anhydrase 7 preincubated for 15 mins by stopped flow CO2 hydration assay | B | 8 | pKi | 10 | nM | Ki | J Med Chem (2016) 59: 6547-6552 [PMID:27305384] |
| carbonic anhydrase 12/Carbonic anhydrase XII in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3242] [GtoPdb: 2747] [UniProtKB: O43570] | ||||||||
| ChEMBL | Inhibition of recombinant human carbonic anhydrase 12 expressed in Escherichia coli L21-GOLD (DE3) incubated for 10 mins prior to testing by stopped-flow CO2 hydration assay | B | 6.19 | pKi | 650 | nM | Ki | J Med Chem (2018) 61: 1176-1181 [PMID:29266943] |
| ChEMBL | Inhibition of human carbonic anhydrase 12 by stopped-flow CO2 hydrase assay | B | 6.2 | pKi | 633 | nM | Ki | Bioorg Med Chem (2014) 22: 1821-1831 [PMID:24560739] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 12 expressed in Escherichia coli by stopped flow CO2 hydration assay | B | 6.2 | pKi | 633 | nM | Ki | J Med Chem (2014) 57: 3522-3531 [PMID:24689792] |
| ChEMBL | Inhibition of human recombinant carbonic anhydrase 12 preincubated for 15 mins by stopped flow CO2 hydration assay | B | 6.2 | pKi | 633 | nM | Ki | Bioorg Med Chem (2016) 24: 1095-1105 [PMID:26810710] |
| ChEMBL | Inhibition of recombinant human carbonic anhydrase-12 assessed as reduction in CO2 hydration preincubated for 10 mins measured for 5 to 10 secs by stopped flow assay | B | 6.2 | pKi | 633 | nM | Ki | Bioorg Med Chem (2017) 25: 3583-3589 [PMID:28416101] |
| ChEMBL | Inhibition of recombinant human carbonic anhydrase 12 incubated for 1 hr prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay | B | 6.2 | pKi | 633 | nM | Ki | J Med Chem (2020) 63: 321-333 [PMID:31794211] |
| ChEMBL | Inhibition of human recombinant CA12 by CO2 hydration stopped flow assay | B | 6.2 | pKi | 633 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 836-841 [PMID:18042384] |
| ChEMBL | Inhibition of human carbonic anhydrase 12 preincubated for 15 mins by stopped flow CO2 hydration assay | B | 6.2 | pKi | 633 | nM | Ki | J Med Chem (2016) 59: 6547-6552 [PMID:27305384] |
| 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 expressed in Escherichia coli by stopped flow CO2 hydration assay | B | 6.11 | pKi | 773 | nM | Ki | J Med Chem (2014) 57: 3522-3531 [PMID:24689792] |
| 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 | 5.04 | pKi | 9200 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 275-279 [PMID:24314394] |
| 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 | 5.1 | pKi | 7960 | nM | Ki | J Med Chem (2009) 52: 3116-3120 [PMID:19338333] |
| TAS2R31 in Human [GtoPdb: 674] [UniProtKB: P59538] | ||||||||
| GtoPdb | - | - | 2.96 | pEC50 | 1100000 | nM | EC50 | J Neurosci (2004) 24: 10260-5 [PMID:15537898] |
| TAS2R43 in Human [GtoPdb: 678] [UniProtKB: P59537] | ||||||||
| GtoPdb | - | - | 2.77 | pEC50 | 1700000 | nM | EC50 | J Neurosci (2004) 24: 10260-5 [PMID:15537898] |
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]
