PF-04457845 [Ligand Id: 6694] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1651534 (Pf-04457845, PF-04457845, PF-4457845, Redafamdastat)
  • α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
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  • Fatty acid amide hydrolase/Anandamide amidohydrolase in Human [ChEMBL: CHEMBL2243] [GtoPdb: 1400] [UniProtKB: O00519]
  • Fatty acid amide hydrolase/Anandamide amidohydrolase in Rat [ChEMBL: CHEMBL3229] [GtoPdb: 1400] [UniProtKB: P97612]
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  • CB1 receptor/Cannabinoid CB1 receptor in Human [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554]
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  • CB2 receptor/Cannabinoid CB2 receptor in Human [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972]
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  • GABAA receptor α1 subunit/GABA receptor alpha-1 subunit in Human [ChEMBL: CHEMBL1962] [GtoPdb: 404] [UniProtKB: P14867]
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
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  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
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  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
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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
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
Fatty acid amide hydrolase/Anandamide amidohydrolase 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 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 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 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]
CB1 receptor/Cannabinoid CB1 receptor 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 CB2 receptor 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
GABAA receptor α1 subunit/GABA receptor alpha-1 subunit 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
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor 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/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 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 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 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 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]