PF-05190457 [Ligand Id: 9060] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3287218 (Pf-05190457, Pf-5190457, PF-5190457) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| ghrelin receptor/Ghrelin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4616] [GtoPdb: 246] [UniProtKB: Q92847] | ||||||||
| ChEMBL | Displacement of [125I]ghrelin from human ghrelin receptor expressed in HEK293 cells after 8 hrs by scintillation proximity assay | B | 8.18 | pKi | 6.61 | nM | Ki | ACS Med Chem Lett (2014) 5: 474-479 [PMID:24900864] |
| ChEMBL | Inverse agonist activity at human ghrelin receptor expressed in HEK293 cells assessed as inhibition of ghrelin-induced europium-labeled GTP-gamma-S binding by DELFIA | B | 8.18 | pKi | 6.61 | nM | Ki | ACS Med Chem Lett (2014) 5: 474-479 [PMID:24900864] |
| GtoPdb | Measured in vitro in recombinant receptor over-expressing cells. | - | 8.85 | pKi | 1.42 | nM | Ki | Br J Pharmacol (2016) 173: 1452-64 [PMID:26784385] |
| ghrelin receptor in Mouse [GtoPdb: 246] [UniProtKB: Q99P50] | ||||||||
| GtoPdb | Measured in vitro in recombinant receptor over-expressing cells | - | 8.11 | pKi | 7.7 | nM | Ki | Br J Pharmacol (2016) 173: 1452-64 [PMID:26784385] |
| ghrelin receptor in Rat [GtoPdb: 246] [UniProtKB: O08725] | ||||||||
| GtoPdb | Measured in vitro in recombinant receptor over-expressing cells | - | 8.49 | pKi | 3.2 | nM | Ki | Br J Pharmacol (2016) 173: 1452-64 [PMID:26784385] |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of human ERG | B | 5.16 | pIC50 | 6900 | nM | IC50 | ACS Med Chem Lett (2014) 5: 474-479 [PMID:24900864] |
| 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
| ChEMBL | Inhibition of 5HT2B receptor (unknown origin) | B | 5.43 | pIC50 | 3700 | nM | IC50 | ACS Med Chem Lett (2014) 5: 474-479 [PMID:24900864] |
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]
