PF-514273 [Ligand Id: 11693] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL484929 (PF-0514273) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| ADGRF1/Adhesion G-protein coupled receptor F1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523872] [GtoPdb: 190] [UniProtKB: Q5T601] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in agonist mode with target: ADGRF1 | F | 5.69 | pEC50 | 2041.85 | nM | EC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: ADRA2A | F | 5.97 | pEC50 | 1060 | nM | EC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| apelin receptor/Apelin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1628481] [GtoPdb: 36] [UniProtKB: P35414] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in agonist mode with target: APLNR | F | 5 | pEC50 | >10000 | nM | EC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| β2-adrenoceptor/Beta-2 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: ADRB2 | F | 5.84 | pEC50 | 1438.21 | nM | EC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| CB1 receptor/Cannabinoid CB1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554] | ||||||||
| ChEMBL | Binding affinity to CB1 receptor | B | 9 | pKi | 1 | nM | Ki | J Med Chem (2009) 52: 2652-2655 [PMID:19351113] |
| ChEMBL | Displacement of [3H]SR141716A form human CB1 receptor expressed in HEK293 cells after 60 mins by beta counting | B | 9 | pKi | 1 | nM | Ki | ACS Med Chem Lett (2012) 3: 397-401 [PMID:24900484] |
| ChEMBL | Antagonist activity at human CB1 receptor expressed in CHOK1 cells assessed as inhibition of CP-55940-induced response after 10 mins by GTPgamma[35S] binding assay | F | 9.09 | pKi | 0.82 | nM | Ki | J Med Chem (2009) 52: 2652-2655 [PMID:19351113] |
| ChEMBL | Antagonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of CP-55940-induced [35S]GTPgammaS binding incubated for 10 mins prior to CP-55940-challenge measured after 1 hr by beta counting | F | 9.09 | pKi | 0.82 | nM | Ki | ACS Med Chem Lett (2012) 3: 397-401 [PMID:24900484] |
| GtoPdb | Antagonism of CP-55940-induced GTPgamma[35S] binding at CB1 expressed in CHOK1 cells | - | 9.09 | pKi | 0.82 | nM | Ki | J Med Chem (2009) 52: 2652-5 [PMID:19351113] |
| CB2 receptor/Cannabinoid CB2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972] | ||||||||
| ChEMBL | Binding affinity to CB2 receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2009) 52: 2652-2655 [PMID:19351113] |
| ChEMBL | Displacement of [3H]CP-55940 from human CB2 receptor expressed in CHO-K1 cells after 60 mins by beta counting | B | 5 | pKi | >10000 | nM | Ki | ACS Med Chem Lett (2012) 3: 397-401 [PMID:24900484] |
| CX3CR1/C-X3-C chemokine receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4843] [GtoPdb: 74] [UniProtKB: P49238] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: CX3CR1 | F | 4.76 | pEC50 | 17564.2 | nM | EC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| GLP-1 receptor/Glucagon-like peptide 1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1784] [GtoPdb: 249] [UniProtKB: P43220] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: GLP1R | F | 5.64 | pEC50 | 2265.15 | nM | EC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| GPR119/Glucose-dependent insulinotropic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5652] [GtoPdb: 126] [UniProtKB: Q8TDV5] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR119 | F | 6.26 | pEC50 | 553.25 | nM | EC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| FFA4 receptor/G-protein coupled receptor 120 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5339] [GtoPdb: 127] [UniProtKB: Q5NUL3] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: FFAR4 | F | 5.92 | pEC50 | 1210.33 | nM | EC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| GPR183/G-protein coupled receptor 183 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3259470] [GtoPdb: 81] [UniProtKB: P32249] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183 | F | 5 | pIC50 | >10000 | nM | IC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| GPR35/G-protein coupled receptor 35 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293267] [GtoPdb: 102] [UniProtKB: Q9HC97] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in agonist mode with target: GPR35 | F | 5 | pEC50 | >10000 | nM | EC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| FPR2/Lipoxin A4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4227] [GtoPdb: 223] [UniProtKB: P25090] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: FPR2 | F | 5 | pIC50 | >10000 | nM | IC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| S1P1 receptor/Sphingosine 1-phosphate receptor Edg-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4333] [GtoPdb: 275] [UniProtKB: P21453] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: S1PR1 | F | 5 | pIC50 | >10000 | nM | IC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| AT1 receptor/Type-1 angiotensin II receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL227] [GtoPdb: 34] [UniProtKB: P30556] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: AGTR1 | F | 5.9 | pEC50 | 1259.37 | nM | EC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
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]
