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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 |
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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 | 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 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]