L-775,606 [Ligand Id: 114] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL292779 (L-775606)
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Mouse [ChEMBL: CHEMBL3737] [GtoPdb: 1] [UniProtKB: Q64264]
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  • 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
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  • 5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
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  • 5-ht1e receptor/Serotonin 1e (5-HT1e) receptor in Human [ChEMBL: CHEMBL2182] [GtoPdb: 4] [UniProtKB: P28566]
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  • 5-HT1F receptor/Serotonin 1f (5-HT1f) receptor in Human [ChEMBL: CHEMBL1805] [GtoPdb: 5] [UniProtKB: P30939]
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
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  • 5-HT3A/Serotonin 3a (5-HT3a) receptor in Human [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3737] [GtoPdb: 1] [UniProtKB: Q64264]
ChEMBL Compound was evaluated for the affinity at 5-hydroxytryptamine 1A receptor B 7.26 pIC50 55 nM IC50 J Med Chem (1997) 40: 3501-3503 [PMID:9357515]
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
GtoPdb - - 6.9 pKi - - - Mol Pharmacol (2000) 58: 1042-9 [PMID:11040052]
ChEMBL Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells B 7.12 pIC50 75 nM IC50 J Med Chem (1997) 40: 3501-3503 [PMID:9357515]
ChEMBL Compound was evaluated for the affinity at 5-hydroxytryptamine 1B receptor B 7.12 pIC50 75 nM IC50 J Med Chem (1997) 40: 3501-3503 [PMID:9357515]
ChEMBL Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells. B 7.14 pIC50 72 nM IC50 J Med Chem (1999) 42: 691-705 [PMID:10052976]
ChEMBL Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells B 7.14 pIC50 72 nM IC50 J Med Chem (1999) 42: 2087-2104 [PMID:10377215]
ChEMBL Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor F 6.37 pEC50 430 nM EC50 J Med Chem (1999) 42: 2087-2104 [PMID:10377215]
5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
ChEMBL Displacement of [3H]5-HT from human 5-hydroxytryptamine 1D receptor expressed in CHO cells B 9.22 pIC50 0.6 nM IC50 J Med Chem (1998) 41: 2667-2670 [PMID:9667955]
ChEMBL Displacement of [3H]5-HT from human 5-hydroxytryptamine 1D receptor expressed in CHO cells B 9.22 pIC50 0.6 nM IC50 J Med Chem (1997) 40: 3501-3503 [PMID:9357515]
ChEMBL Compound was evaluated for the affinity at 5-hydroxytryptamine 1D receptor B 9.22 pIC50 0.6 nM IC50 J Med Chem (1997) 40: 3501-3503 [PMID:9357515]
ChEMBL Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1D receptor expressed in CHOK1 cells by liquid scintillation counting B 9.22 pIC50 0.6 nM IC50 J Med Chem (2008) 51: 3609-3616 [PMID:18507369]
ChEMBL Displacement of [3H]5-HT binding to the cloned human 5-hydroxytryptamine 1D receptor stably expressed in CHO cells B 9.3 pIC50 0.5 nM IC50 J Med Chem (1999) 42: 691-705 [PMID:10052976]
ChEMBL Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1D receptor expressed in CHO cells B 9.3 pIC50 0.5 nM IC50 J Med Chem (1999) 42: 2087-2104 [PMID:10377215]
ChEMBL Agonist induced [35S]GTP-gamma-S, binding in CHO cells expressing 5-HT 1d receptor F 8.92 pEC50 1.2 nM EC50 J Med Chem (1998) 41: 2667-2670 [PMID:9667955]
ChEMBL Compound was evaluated for the stimulation of [35S]GTP-gamma-S, binding in CHO cells expressing the 5-hydroxytryptamine 1D receptor. F 8.92 pEC50 1.2 nM EC50 J Med Chem (1997) 40: 3501-3503 [PMID:9357515]
ChEMBL Stimulation of [35S]GTP-gamma-S, binding in CHO cells expressing the human 5-hydroxytryptamine 1D receptor. F 9 pEC50 1 nM EC50 J Med Chem (1999) 42: 691-705 [PMID:10052976]
ChEMBL Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1D receptor F 9 pEC50 1 nM EC50 J Med Chem (1999) 42: 2087-2104 [PMID:10377215]
5-ht1e receptor/Serotonin 1e (5-HT1e) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2182] [GtoPdb: 4] [UniProtKB: P28566]
ChEMBL Compound was evaluated for the affinity at 5-hydroxytryptamine 1E receptor B 5 pIC50 >10000 nM IC50 J Med Chem (1997) 40: 3501-3503 [PMID:9357515]
5-HT1F receptor/Serotonin 1f (5-HT1f) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1805] [GtoPdb: 5] [UniProtKB: P30939]
ChEMBL Compound was evaluated for the affinity at 5-hydroxytryptamine 1F receptor B 5.42 pIC50 3800 nM IC50 J Med Chem (1997) 40: 3501-3503 [PMID:9357515]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL Compound was evaluated for the affinity at 5-hydroxytryptamine 2A receptor B 6.43 pIC50 370 nM IC50 J Med Chem (1997) 40: 3501-3503 [PMID:9357515]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL Compound was evaluated for the affinity at 5-hydroxytryptamine 2C receptor B 5.05 pIC50 9000 nM IC50 J Med Chem (1997) 40: 3501-3503 [PMID:9357515]
5-HT3A/Serotonin 3a (5-HT3a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098]
ChEMBL Compound was evaluated for the affinity at 5-hydroxytryptamine 3 receptor B 5 pIC50 >10000 nM IC50 J Med Chem (1997) 40: 3501-3503 [PMID:9357515]

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]