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ChEMBL ligand: CHEMBL19224 (NSC-136630, Papaverine, Papaverinum) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Acetylcholinesterase in Electrophorus electricus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4078] [UniProtKB: O42275] | ||||||||
ChEMBL | Inhibition of Electrophorus electricus (electric eel) acetylcholinesterase (AChE) using acetylcholine iodide as substrate by Ellman method | B | 4.61 | pIC50 | 24300 | nM | IC50 | Med Chem Res (2009) 18: 231-241 |
acetylcholinesterase (Yt blood group)/Acetylcholinesterase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL220] [GtoPdb: 2465] [UniProtKB: P22303] | ||||||||
ChEMBL | Inhibition of AChE activity | B | 4.61 | pIC50 | 24330 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 2170-2172 [PMID:16483771] |
phosphodiesterase 10A in Human [GtoPdb: 1310] [UniProtKB: Q9Y233] | ||||||||
GtoPdb | - | - | 7.68 | pIC50 | 21 | nM | IC50 | Eur J Med Chem (2011) 46: 3986-95 [PMID:21705115] |
GtoPdb | - | - | 7.77 | pIC50 | 17 | nM | IC50 | Bioorg Med Chem (2011) 19: 642-9 [PMID:21087867] |
phosphodiesterase 10A/cAMP and cAMP-inhibited cGMP 3`,5`-cyclic phosphodiesterase 10A in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6140] [GtoPdb: 1310] [UniProtKB: Q9QYJ6] | ||||||||
ChEMBL | Inhibition of rat PDE10A | B | 7.44 | pIC50 | 36 | nM | IC50 | Eur J Med Chem (2011) 46: 3986-3995 [PMID:21705115] |
ChEMBL | Competitive inhibition of rat recombinant PDE10A by scintillation proximity assay in presence of cAMP | B | 7.44 | pIC50 | 36 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 197-202 [PMID:26597534] |
ChEMBL | Inhibition of recombinant rat PDE10A expressed in Sf9 insect cells using cGMP or cAMP as substrate by scintillation proximity assay | B | 7.44 | pIC50 | 36 | nM | IC50 | Eur J Med Chem (2018) 150: 742-756 [PMID:29574203] |
ChEMBL | Inhibition of recombinant rat PDE10A expressed in Sf9 cells using cGMP/cAMP as substrate by scintillation proximity assay | B | 7.44 | pIC50 | 36 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 1419-1422 [PMID:30952590] |
CYP2C19/Cytochrome P450 2C19 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3622] [GtoPdb: 1328] [UniProtKB: P33261] | ||||||||
ChEMBL | DRUGMATRIX: CYP450, 2C19 enzyme inhibition (substrate: 3-Cyano-7-ethoxycoumarin) | B | 6.12 | pIC50 | 762 | nM | IC50 | DrugMatrix in vitro pharmacology data |
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
ChEMBL | Inhibition of human ERG | B | 5.14 | pIC50 | 7244.36 | nM | IC50 | Eur J Med Chem (2011) 46: 618-630 [PMID:21185626] |
phosphodiesterase 10A/Phosphodiesterase 10A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4409] [GtoPdb: 1310] [UniProtKB: Q9Y233] | ||||||||
ChEMBL | Inhibition of PDE10A (unknown origin) | B | 6.68 | pIC50 | 210 | nM | IC50 | Bioorg Med Chem (2013) 21: 6053-6062 [PMID:23978358] |
ChEMBL | Inhibition of PDE10A | B | 6.68 | pIC50 | 210 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3738-3742 [PMID:21602043] |
ChEMBL | Inhibition of human MOLT4 cell-derived PDE10A using [3H]cAMP as substrate measured after 2 hrs in presence of rolipram/milrinone by topcount method | B | 7.01 | pIC50 | 97 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 1419-1422 [PMID:30952590] |
ChEMBL | Inhibition of recombinant full length human PDE10A by scintillation proximity assay in presence of cAMP | B | 7.03 | pIC50 | 92.3 | nM | IC50 | Medchemcomm (2015) 6: 2063-2080 |
ChEMBL | Inhibition of human recombinant PDE10A expressed in baculovirus-SF21 cell system assessed as hydrolysis of [3H]cAMP after 1 hr by liquid scintillation counting | B | 7.12 | pIC50 | 76 | nM | IC50 | J Med Chem (2010) 53: 4399-4411 [PMID:20450197] |
ChEMBL | Inhibition of human recombinant PDE10A expressed in baculovirus-SF21 cell system assessed as hydrolysis of [3H]cAMP after 1 hr by liquid scintillation counting | B | 7.24 | pIC50 | 56.9 | nM | IC50 | J Med Chem (2010) 53: 4399-4411 [PMID:20450197] |
ChEMBL | Inhibition of PDE10A | B | 7.4 | pIC50 | 40 | nM | IC50 | J Med Chem (2012) 55: 7299-7331 [PMID:22834877] |
ChEMBL | Inhibition of human recombinant full length PDE10A using cAMP as substrate preincubated for 20 mins measured after 4 hrs | B | 7.44 | pIC50 | 36 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 1944-1948 [PMID:22321214] |
ChEMBL | Inhibition of PDE10A (unknown origin) | B | 7.44 | pIC50 | 36 | nM | IC50 | Bioorg Med Chem (2014) 22: 2648-2654 [PMID:24721831] |
ChEMBL | Binding affinity to PDE10A (unknown origin) | B | 7.44 | pIC50 | 36 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 919-924 [PMID:25592707] |
ChEMBL | Inhibition of PDE10A (unknown origin) | B | 7.44 | pIC50 | 36 | nM | IC50 | J Med Chem (2021) 64: 7083-7109 [PMID:34042442] |
ChEMBL | Inhibition of PDE10A (unknown origin) | B | 7.44 | pIC50 | 36 | nM | IC50 | Bioorg Med Chem (2019) 27: 3440-3450 [PMID:31235264] |
ChEMBL | Inhibition of human recombinant PDE10A assessed as reduction in hydrolysis of [3H]cAMP by scintillation proximity assay | B | 7.68 | pIC50 | 21 | nM | IC50 | Eur J Med Chem (2011) 46: 3986-3995 [PMID:21705115] |
GtoPdb | - | - | 7.68 | pIC50 | 21 | nM | IC50 | Eur J Med Chem (2011) 46: 3986-95 [PMID:21705115] |
ChEMBL | Inhibition of human PDE10A expressed in Sf9 cells using [3H]cAMP by scintillation proximity assay | B | 7.77 | pIC50 | 17 | nM | IC50 | Bioorg Med Chem (2011) 19: 642-649 [PMID:21087867] |
GtoPdb | - | - | 7.77 | pIC50 | 17 | nM | IC50 | Bioorg Med Chem (2011) 19: 642-9 [PMID:21087867] |
phosphodiesterase 2A/Phosphodiesterase 2A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2652] [GtoPdb: 1297] [UniProtKB: O00408] | ||||||||
ChEMBL | Inhibition of cyclic GMP sensitive phosphodiesterase PDE 2 of human lung | B | 4.77 | pIC50 | 17000 | nM | IC50 | J Med Chem (1985) 28: 537-545 [PMID:2985781] |
ChEMBL | Inhibition of cGMP-stimulated phosphodiesterase 2 of porcine coronary arteries | B | 5.64 | pIC50 | 2300 | nM | IC50 | J Med Chem (1993) 36: 3765-3770 [PMID:8254606] |
phosphodiesterase 3A/Phosphodiesterase 3A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL241] [GtoPdb: 1298] [UniProtKB: Q14432] | ||||||||
ChEMBL | Inhibition of human recombinant PDE3A transfected in Sf9 cells by SPA | B | 6.55 | pKi | 279 | nM | Ki | J Med Chem (2007) 50: 182-185 [PMID:17228859] |
ChEMBL | Inhibition of PDE3A (unknown origin) | B | 5.89 | pIC50 | 1300 | nM | IC50 | Bioorg Med Chem (2019) 27: 3440-3450 [PMID:31235264] |
ChEMBL | Inhibition of PDE3A assessed as reduction in hydrolysis of [3H]cAMP by scintillation proximity assay | B | 6.04 | pIC50 | 917 | nM | IC50 | Eur J Med Chem (2011) 46: 3986-3995 [PMID:21705115] |
GtoPdb | - | - | 6.04 | pIC50 | 917 | nM | IC50 | Eur J Med Chem (2011) 46: 3986-95 [PMID:21705115] |
ChEMBL | Inhibition of PDE3A (unknown origin) | B | 6.54 | pIC50 | 287 | nM | IC50 | J Med Chem (2019) 62: 3707-3721 [PMID:30888810] |
ChEMBL | Inhibition of PDE3A | B | 6.55 | pIC50 | 284 | nM | IC50 | J Med Chem (2012) 55: 7299-7331 [PMID:22834877] |
Phosphodiesterase 3A in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3061] [UniProtKB: Q9XSW7] | ||||||||
ChEMBL | Inhibition of cGMP-inhibited phosphodiesterase from porcine coronary arteries | B | 6.21 | pIC50 | 620 | nM | IC50 | J Med Chem (1993) 36: 3765-3770 [PMID:8254606] |
phosphodiesterase 3B/Phosphodiesterase 3B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL290] [GtoPdb: 1299] [UniProtKB: Q13370] | ||||||||
ChEMBL | Inhibition of human recombinant PDE3B transfected in Sf9 cells by SPA | B | 6.38 | pKi | 417 | nM | Ki | J Med Chem (2007) 50: 182-185 [PMID:17228859] |
ChEMBL | Inhibition of PDE3B assessed as reduction in hydrolysis of [3H]cAMP by scintillation proximity assay | B | 5.99 | pIC50 | 1030 | nM | IC50 | Eur J Med Chem (2011) 46: 3986-3995 [PMID:21705115] |
GtoPdb | - | - | 5.99 | pIC50 | 1030 | nM | IC50 | Eur J Med Chem (2011) 46: 3986-95 [PMID:21705115] |
phosphodiesterase 4A/Phosphodiesterase 4A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL254] [GtoPdb: 1300] [UniProtKB: P27815] | ||||||||
ChEMBL | Inhibition of PDE4A (unknown origin) | B | 5.8 | pIC50 | 1600 | nM | IC50 | J Med Chem (2019) 62: 3707-3721 [PMID:30888810] |
Phosphodiesterase 4A in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3333] [UniProtKB: O77823] | ||||||||
ChEMBL | Inhibition of cAMP specific phosphodiesterase from porcine coronary arteries | B | 5.77 | pIC50 | 1700 | nM | IC50 | J Med Chem (1993) 36: 3765-3770 [PMID:8254606] |
phosphodiesterase 4D/Phosphodiesterase 4D in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL288] [GtoPdb: 1303] [UniProtKB: Q08499] | ||||||||
ChEMBL | Inhibition of PDE4D (unknown origin) | B | 5.85 | pIC50 | 1400 | nM | IC50 | J Med Chem (2016) 59: 7029-7065 [PMID:26908025] |
phosphodiesterase 5A/Phosphodiesterase 5A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1827] [GtoPdb: 1304] [UniProtKB: O76074] | ||||||||
ChEMBL | Inhibitory activity against cyclic GMP-phosphodiesterase (PDE V) isolated from porcine aorta. | B | 5.06 | pIC50 | 8800 | nM | IC50 | J Med Chem (1993) 36: 3765-3770 [PMID:8254606] |
Serine hydroxymethyltransferase, mitochondrial in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4295747] [UniProtKB: P34897] | ||||||||
ChEMBL | Inhibition of His-tagged human recombinant SHMT2 expressed in Escherichia coli BLR(DE3) assessed as reduction in NADPH level using L-serine, THF and NADP+ incubated for 5 mins by SHMT2-MTHFD coupled reaction based fluorescence assay | B | 5.57 | pIC50 | 2691.53 | nM | IC50 | WO-2016085990-A1. Compositions and methods relating to inhibiting serine hyrdoxymethyltransferase 2 activity (2016) |
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]