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 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]
