PF-03654746 [Ligand Id: 9058] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2151197 (Pf-03654746, PF 03654746) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| H3 receptor/Histamine H3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1] | ||||||||
| ChEMBL | Displacement of [3H]-n-alpha-methylhistamine from human histamine H3 receptor homogenate after 60 mins by scintillation counting | B | 8.64 | pKi | 2.3 | nM | Ki | J Med Chem (2011) 54: 7602-7620 [PMID:21928839] |
| ChEMBL | Displacement of [3H]-n-alpha-methylhistamine from human histamine H3 receptor homogenate after 60 mins by scintillation counting | B | 8.64 | pKi | 2.29 | nM | Ki | J Med Chem (2011) 54: 7602-7620 [PMID:21928839] |
| GtoPdb | - | - | 8.64 | pKi | 2.3 | nM | Ki | J Med Chem (2011) 54: 7602-20 [PMID:21928839] |
| ChEMBL | Antagonist activity at human histamine H3 receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP release pretreated 10 mins prior forskolin stimulation measured after 4.5 hrs by spectrofluorimetric analysis | F | 8.77 | pKi | 1.7 | nM | Ki | J Med Chem (2011) 54: 7602-7620 [PMID:21928839] |
| ChEMBL | Antagonist activity at human histamine H3 receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP release pretreated 10 mins prior forskolin stimulation measured after 4.5 hrs by spectrofluorimetric analysis | F | 8.77 | pKi | 1.7 | nM | Ki | J Med Chem (2011) 54: 7602-7620 [PMID:21928839] |
| H3 receptor in Mouse [GtoPdb: 264] [UniProtKB: P58406] | ||||||||
| GtoPdb | - | - | 7.43 | pKi | 37 | nM | Ki | J Med Chem (2011) 54: 7602-20 [PMID:21928839] |
| H3 receptor/Histamine H3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4124] [GtoPdb: 264] [UniProtKB: Q9QYN8] | ||||||||
| ChEMBL | Displacement of [3H]-n-alpha-methylhistamine from rat histamine H3 receptor homogenate after 60 mins by scintillation counting | B | 7.43 | pKi | 37.15 | nM | Ki | J Med Chem (2011) 54: 7602-7620 [PMID:21928839] |
| ChEMBL | Displacement of [3H]-n-alpha-methylhistamine from rat histamine H3 receptor homogenate after 60 mins by scintillation counting | B | 7.43 | pKi | 37 | nM | Ki | J Med Chem (2011) 54: 7602-7620 [PMID:21928839] |
| ChEMBL | Antagonist activity at rat histamine H3 receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP release pretreated 10 mins prior forskolin stimulation measured after 4.5 hrs by spectrofluorimetric analysis | F | 8.05 | pKi | 8.91 | nM | Ki | J Med Chem (2011) 54: 7602-7620 [PMID:21928839] |
| ChEMBL | Antagonist activity at rat histamine H3 receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP release pretreated 10 mins prior forskolin stimulation measured after 4.5 hrs by spectrofluorimetric analysis | F | 8.05 | pKi | 8.9 | nM | Ki | J Med Chem (2011) 54: 7602-7620 [PMID:21928839] |
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]
