papaverine [Ligand Id: 13147] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL19224 (NSC-136630, Papaverine, Papaverinum) |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 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 | B | 6.68 | pIC50 | 210 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3738-3742 [PMID:21602043] |
| 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 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 | 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 (null) |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]
