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 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]