PF-04995274 [Ligand Id: 9059] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2152922 (Pf-04995274) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1875] [GtoPdb: 9] [UniProtKB: Q13639] | ||||||||
| ChEMBL | Displacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting | B | 9.34 | pKi | 0.46 | nM | Ki | J Med Chem (2012) 55: 9240-9254 [PMID:22974325] |
| ChEMBL | Displacement of [3H]GR113808 from human 5HT4A receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting | B | 9.44 | pKi | 0.36 | nM | Ki | J Med Chem (2012) 55: 9240-9254 [PMID:22974325] |
| ChEMBL | Displacement of [3H]GR113808 from human 5HT4E receptor expressed in CHO cells after 30 mins by liquid scintillation counting | B | 9.49 | pKi | 0.32 | nM | Ki | J Med Chem (2012) 55: 9240-9254 [PMID:22974325] |
| GtoPdb | Measured at the 5-HT4d receptor. | - | 9.82 | pKi | 0.15 | nM | Ki | J Med Chem (2012) 55: 9240-54 [PMID:22974325] |
| ChEMBL | Displacement of [3H]GR113808 from human 5HT4D receptor expressed in HEK293 cells after 30 mins by liquid scintillation counting | B | 9.82 | pKi | 0.15 | nM | Ki | J Med Chem (2012) 55: 9240-9254 [PMID:22974325] |
| ChEMBL | Agonist activity at recombinant human 5-HT4E receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assay | B | 8.82 | pEC50 | 1.5 | nM | EC50 | J Med Chem (2018) 61: 4993-5008 [PMID:29763304] |
| ChEMBL | Partial agonist activity at human 5HT4E receptor expressed in CHO cells assessed as cAMP accumulation incubated for 4 hrs by luciferase reporter gene luminescence assay | B | 8.89 | pEC50 | 1.3 | nM | EC50 | J Med Chem (2021) 64: 10641-10665 [PMID:34251799] |
| ChEMBL | Agonist activity at human 5HT4e receptor expressed in CHO cells assessed as cAMP level after 4 hrs by luciferase reporter gene assay | F | 8.89 | pEC50 | 1.3 | nM | EC50 | Eur J Med Chem (2015) 103: 289-301 [PMID:26363507] |
| ChEMBL | Agonist activity at human 5HT4A receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay | F | 9.33 | pEC50 | 0.47 | nM | EC50 | J Med Chem (2012) 55: 9240-9254 [PMID:22974325] |
| ChEMBL | Agonist activity at human 5HT4B receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay | F | 9.44 | pEC50 | 0.36 | nM | EC50 | J Med Chem (2012) 55: 9240-9254 [PMID:22974325] |
| ChEMBL | Agonist activity at 5-HT4E receptor (unknown origin) | B | 9.59 | pEC50 | 0.26 | nM | EC50 | J Med Chem (2018) 61: 4993-5008 [PMID:29763304] |
| ChEMBL | Agonist activity at human 5HT4E receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay | F | 9.59 | pEC50 | 0.26 | nM | EC50 | J Med Chem (2012) 55: 9240-9254 [PMID:22974325] |
| ChEMBL | Partial agonist activity at human 5HT4D receptor expressed in HEK293 cells assessed as cAMP production after 30 mins by HTRF assay | F | 9.7 | pEC50 | 0.2 | nM | EC50 | J Med Chem (2012) 55: 9240-9254 [PMID:22974325] |
| 5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4317] [GtoPdb: 9] [UniProtKB: Q62758] | ||||||||
| ChEMBL | Displacement of [3H]GR113808 from 5HT4 receptor in rat striatal membrane after 30 mins by liquid scintillation counting | B | 9.52 | pKi | 0.3 | nM | Ki | J Med Chem (2012) 55: 9240-9254 [PMID:22974325] |
| ChEMBL | Agonist activity at rat 5HT4L receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay | F | 9.19 | pEC50 | 0.65 | nM | EC50 | J Med Chem (2012) 55: 9240-9254 [PMID:22974325] |
| ChEMBL | Agonist activity at rat 5HT4E receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay | F | 9.21 | pEC50 | 0.62 | nM | EC50 | J Med Chem (2012) 55: 9240-9254 [PMID:22974325] |
| ChEMBL | Agonist activity at rat 5HT4S receptor expressed in HEK293 cells assessed as increase in cAMP production after 30 mins by HTRF assay | F | 9.23 | pEC50 | 0.59 | nM | EC50 | J Med Chem (2012) 55: 9240-9254 [PMID:22974325] |
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]
