PF-04457845 [Ligand Id: 6694] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1651534 (Pf-04457845, PF-4457845, Redafamdastat) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 5-HT2A receptor/5-hydroxytryptamine receptor 2A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| ChEMBL | 5-HT2A (h) (agonist site) CEREP ligand profiling | B | 5.8 | pKi | 1600 | nM | Ki | Data for DCP probe PF-04457845 |
| ChEMBL | Selectivity interaction (CEREP ligand profiling panel (ion channels, GPCRS and transporters)) EUB0000306b HTR2A | B | 5.8 | pKi | 1600 | nM | Ki | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| ChEMBL | GPCRScan assay: inhibition of 5-HT2A | B | 6.6 | pKi | 251.19 | nM | Ki | Data for DCP probe PF-04457845 |
| ChEMBL | GPCRScan assay: inhibition of 5-HT2A | B | 6.6 | pKi | 248.71 | nM | Ki | Data for DCP probe PF-04457845 |
| ChEMBL | Selectivity interaction (GPCR panel (PDSP screen)) EUB0000306b HTR2A | B | 6.6 | pKi | 248.71 | nM | Ki | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| 5-HT2B receptor/5-hydroxytryptamine receptor 2B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
| ChEMBL | GPCRScan assay: inhibition of 5-HT2B | B | 5.87 | pKi | 1348.96 | nM | Ki | Data for DCP probe PF-04457845 |
| ChEMBL | GPCRScan assay: inhibition of 5-HT2B | B | 5.87 | pKi | 1338.44 | nM | Ki | Data for DCP probe PF-04457845 |
| 5-HT2C receptor/5-hydroxytryptamine receptor 2C in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| ChEMBL | GPCRScan assay: inhibition of 5-HT2C | B | 5.78 | pKi | 1659.59 | nM | Ki | Data for DCP probe PF-04457845 |
| ChEMBL | GPCRScan assay: inhibition of 5-HT2C | B | 5.78 | pKi | 1659.2 | nM | Ki | Data for DCP probe PF-04457845 |
| α2C-adrenoceptor/Alpha-2C adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825] | ||||||||
| ChEMBL | GPCRScan assay: inhibition of Alpha2C | B | 6.22 | pKi | 602.56 | nM | Ki | Data for DCP probe PF-04457845 |
| ChEMBL | GPCRScan assay: inhibition of Alpha2C | B | 6.23 | pKi | 595.66 | nM | Ki | Data for DCP probe PF-04457845 |
| ChEMBL | Selectivity interaction (GPCR panel (PDSP screen)) EUB0000306b ADRA2C | B | 6.23 | pKi | 595.66 | nM | Ki | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| CB1 receptor/Cannabinoid receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554] | ||||||||
| ChEMBL | CB1 (h) CEREP ligand profiling | B | 4.85 | pKi | 14000 | nM | Ki | Data for DCP probe PF-04457845 |
| CB2 receptor/Cannabinoid receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972] | ||||||||
| ChEMBL | CB2 (h) CEREP ligand profiling | B | 5.29 | pKi | 5100 | nM | Ki | Data for DCP probe PF-04457845 |
| Fatty acid amide hydrolase/Fatty-acid amide hydrolase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2243] [GtoPdb: 1400] [UniProtKB: O00519] | ||||||||
| ChEMBL | Selectivity interaction (HERG functional (IKr) voltage clamp assay) EUB0000306b FAAH | B | 5.33 | pIC50 | 4700 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| ChEMBL | Glutamate dehydrogenase-coupled FAAH assay (preincubation time 1 min) | B | 7.3 | pIC50 | 50.4 | nM | IC50 | Data for DCP probe PF-04457845 |
| ChEMBL | Inhibition of human FAAH assessed as kinact/Ki ratio incubated for 1 min in presence of glutamate dehydrogenase by 384-well format microplate reader assay | B | 7.3 | pIC50 | 50.4 | nM | IC50 | J Pharmacol Exp Ther (2011) 338: 114-124 [PMID:21505060] |
| ChEMBL | Glutamate dehydrogenase-coupled FAAH assay (preincubation time 15 min) | B | 7.49 | pIC50 | 32.4 | nM | IC50 | Data for DCP probe PF-04457845 |
| ChEMBL | Inhibition of human FAAH assessed as kinact/Ki ratio incubated for 15 min in presence of glutamate dehydrogenase by 384-well format microplate reader assay | B | 7.49 | pIC50 | 32.4 | nM | IC50 | J Pharmacol Exp Ther (2011) 338: 114-124 [PMID:21505060] |
| ChEMBL | Glutamate dehydrogenase-coupled FAAH assay (preincubation time 30 min) | B | 7.97 | pIC50 | 10.7 | nM | IC50 | Data for DCP probe PF-04457845 |
| ChEMBL | Inhibition of human FAAH assessed as kinact/Ki ratio incubated for 30 min in presence of glutamate dehydrogenase by 384-well format microplate reader assay | B | 7.97 | pIC50 | 10.7 | nM | IC50 | J Pharmacol Exp Ther (2011) 338: 114-124 [PMID:21505060] |
| ChEMBL | Glutamate dehydrogenase-coupled FAAH assay (preincubation time 60 min) | B | 8.13 | pIC50 | 7.4 | nM | IC50 | Data for DCP probe PF-04457845 |
| GtoPdb | - | - | 8.14 | pIC50 | 7.2 | nM | IC50 | J Pharmacol Exp Ther (2011) 338: 114-24 [PMID:21505060] |
| ChEMBL | Inhibition of human FAAH assessed as kinact/Ki ratio incubated for 60 min in presence of glutamate dehydrogenase by 384-well format microplate reader assay | B | 8.14 | pIC50 | 7.2 | nM | IC50 | J Pharmacol Exp Ther (2011) 338: 114-124 [PMID:21505060] |
| ChEMBL | Affinity Biochemical interaction (Glutamate dehydrogenase-coupled FAAH assay (preincubation time 60 min)) EUB0000306b FAAH | B | 8.14 | pIC50 | 7.2 | nM | IC50 | Affinity Biochemical Literature for EUbOPEN Chemogenomics Library wave 3 |
| ChEMBL | Inhibition of His-tagged human FAAH N-terminal transmembrane-deleted truncated form expressed in Escherichia coli preincubated for 60 mins before oleamide substrate addition | B | 8.14 | pIC50 | 7.2 | nM | IC50 | ACS Med Chem Lett (2011) 2: 91-96 [PMID:21666860] |
| ChEMBL | Inhibition of human transmembrane domain deficient FFAH expressed in Escherichia coli using AAMCA as substrate incubated for 1 min measured for 50 mins by fluorescence assay | B | 8.74 | pIC50 | 1.8 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 238-243 [PMID:30503633] |
| GtoPdb | Inhibition of human FAAH in vitro. | - | 9 | pIC50 | 1 | nM | IC50 |
ACS Med Chem Lett (2011) 2: 91-96 [PMID:21666860]; Science (2017) 356: 1084-1087 [PMID:28596366] |
| Fatty acid amide hydrolase/Fatty-acid amide hydrolase 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3229] [GtoPdb: 1400] [UniProtKB: P97612] | ||||||||
| ChEMBL | Inhibition of rat FAAH assessed as kinact/Ki ratio incubated for 1 min in presence of glutamate dehydrogenase by 384-well format microplate reader assay | B | 7.37 | pIC50 | 43.1 | nM | IC50 | J Pharmacol Exp Ther (2011) 338: 114-124 [PMID:21505060] |
| ChEMBL | Inhibition of rat FAAH assessed as kinact/Ki ratio incubated for 15 min in presence of glutamate dehydrogenase by 384-well format microplate reader assay | B | 7.57 | pIC50 | 26.7 | nM | IC50 | J Pharmacol Exp Ther (2011) 338: 114-124 [PMID:21505060] |
| ChEMBL | Inhibition of rat FAAH assessed as kinact/Ki ratio incubated for 30 min in presence of glutamate dehydrogenase by 384-well format microplate reader assay | B | 7.95 | pIC50 | 11.1 | nM | IC50 | J Pharmacol Exp Ther (2011) 338: 114-124 [PMID:21505060] |
| ChEMBL | Irreversible inhibition of His-tagged rat FAAH N-terminal transmembrane-deleted truncated form expressed in Escherichia coli preincubated for 60 mins before oleamide substrate addition | B | 8.13 | pIC50 | 7.4 | nM | IC50 | ACS Med Chem Lett (2011) 2: 91-96 [PMID:21666860] |
| ChEMBL | Inhibition of rat FAAH assessed as kinact/Ki ratio incubated for 60 min in presence of glutamate dehydrogenase by 384-well format microplate reader assay | B | 8.13 | pIC50 | 7.4 | nM | IC50 | J Pharmacol Exp Ther (2011) 338: 114-124 [PMID:21505060] |
| ChEMBL | Inhibition of rat FFAH expressed in Escherichia coli using AAMCA as substrate incubated for 1 min measured for 50 mins by fluorescence assay | B | 8.24 | pIC50 | 5.7 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 238-243 [PMID:30503633] |
| GABAA receptor α1 subunit/Gamma-aminobutyric acid receptor subunit alpha-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1962] [GtoPdb: 404] [UniProtKB: P14867] | ||||||||
| ChEMBL | Selectivity interaction (GPCR panel (PDSP screen)) EUB0000306b GABRA1 | B | 5.94 | pKi | 1140.08 | nM | Ki | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| σ2/Sigma intracellular receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105907] [GtoPdb: 2553] [UniProtKB: Q5BJF2] | ||||||||
| ChEMBL | GPCRScan assay: inhibition of Sigma 2 | B | 6.36 | pKi | 436.72 | nM | Ki | Data for DCP probe PF-04457845 |
| ChEMBL | Selectivity interaction (GPCR panel (PDSP screen)) EUB0000306b TMEM97 | B | 6.36 | pKi | 436.72 | nM | Ki | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| ChEMBL | GPCRScan assay: inhibition of Sigma 2 | B | 6.36 | pKi | 436.52 | nM | Ki | Data for DCP probe PF-04457845 |
| sigma non-opioid intracellular receptor 1/Sigma non-opioid intracellular receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720] | ||||||||
| ChEMBL | GPCRScan assay: inhibition of Sigma 1 | B | 6.33 | pKi | 472.06 | nM | Ki | Data for DCP probe PF-04457845 |
| ChEMBL | Selectivity interaction (GPCR panel (PDSP screen)) EUB0000306b SIGMAR1 | B | 6.33 | pKi | 472.06 | nM | Ki | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| ChEMBL | GPCRScan assay: inhibition of Sigma 1 | B | 6.33 | pKi | 467.74 | nM | Ki | Data for DCP probe PF-04457845 |
ChEMBL data shown on this page come from version 36:
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]
