PF-04457845 [Ligand Id: 6694] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1651534 (Pf-04457845, PF-04457845, PF-4457845) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 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 |
| Fatty acid amide hydrolase/Anandamide amidohydrolase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2243] [GtoPdb: 1400] [UniProtKB: O00519] | ||||||||
| 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 | Glutamate dehydrogenase-coupled FAAH assay (preincubation time 15 min) | B | 7.49 | pIC50 | 32.4 | nM | IC50 | Data for DCP probe PF-04457845 |
| 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 | Glutamate dehydrogenase-coupled FAAH assay (preincubation time 60 min) | B | 8.13 | pIC50 | 7.4 | nM | IC50 | Data for DCP probe PF-04457845 |
| 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/Anandamide amidohydrolase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3229] [GtoPdb: 1400] [UniProtKB: P97612] | ||||||||
| 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 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] |
| Translocator protein/Peripheral-type benzodiazepine receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4552] [GtoPdb: 2879] [UniProtKB: P16257] | ||||||||
| ChEMBL | GPCRScan assay: inhibition of GABA/PBR | B | 5.94 | pKi | 1148.15 | nM | Ki | Data for DCP probe PF-04457845 |
| ChEMBL | GPCRScan assay: inhibition of GABA/PBR | B | 5.94 | pKi | 1140.08 | nM | Ki | Data for DCP probe PF-04457845 |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| 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 |
| 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor 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/Serotonin 2c (5-HT2c) receptor 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 |
| 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 | 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 opioid receptor 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 | 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 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]
