L-772,405 [Ligand Id: 16] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL313714
  • 5-HT1A receptor/5-hydroxytryptamine receptor 1A in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
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  • 5-HT1B receptor/5-hydroxytryptamine receptor 1B in Human [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
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  • 5-HT1D receptor/5-hydroxytryptamine receptor 1D in Human [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
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  • 5-ht1e receptor/5-hydroxytryptamine receptor 1E in Human [ChEMBL: CHEMBL2182] [GtoPdb: 4] [UniProtKB: P28566]
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  • 5-HT1F receptor/5-hydroxytryptamine receptor 1F in Human [ChEMBL: CHEMBL1805] [GtoPdb: 5] [UniProtKB: P30939]
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  • 5-HT2A receptor/5-hydroxytryptamine receptor 2A in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
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  • 5-HT5A receptor/5-hydroxytryptamine receptor 5A in Human [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898]
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  • 5-HT6 receptor/5-hydroxytryptamine receptor 6 in Rat [ChEMBL: CHEMBL3372] [GtoPdb: 11] [UniProtKB: P31388]
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  • 5-HT7 receptor/5-hydroxytryptamine receptor 7 in Rat [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
5-HT1A receptor/5-hydroxytryptamine receptor 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL Compound was tested for the displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1A receptor stably expressed in CHO cells B 7.18 pIC50 66 nM IC50 J Med Chem (1999) 42: 4981-5001 [PMID:10585208]
GtoPdb - - 7.2 pIC50 - - - J Med Chem (1999) 42: 4981-5001 [PMID:10585208]
5-HT1B receptor/5-hydroxytryptamine receptor 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
ChEMBL Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement. B 6.73 pIC50 185 nM IC50 J Med Chem (1997) 40: 3497-3500 [PMID:9357514]
GtoPdb - - 6.8 pIC50 - - - J Med Chem (1999) 42: 4981-5001 [PMID:10585208]
ChEMBL Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells B 6.82 pIC50 150 nM IC50 J Med Chem (1999) 42: 4981-5001 [PMID:10585208]
5-HT1D receptor/5-hydroxytryptamine receptor 1D 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 Chinese hamster ovary cells (CHO cells) B 9.05 pKi 0.9 nM Ki Bioorg Med Chem Lett (2003) 13: 4409-4413 [PMID:14643336]
GtoPdb - - 9 pIC50 - - - J Med Chem (1999) 42: 4981-5001 [PMID:10585208]
ChEMBL Displacement of [3H]5-HT from human 5-hydroxytryptamine 1D receptor expressed in CHO cells B 9.05 pIC50 0.9 nM IC50 J Med Chem (1998) 41: 2667-2670 [PMID:9667955]
ChEMBL Binding affinity by displacement to human cloned 5-hydroxytryptamine 1D receptor in CHO cells by [3H]5-HT displacement. B 9.05 pIC50 0.9 nM IC50 J Med Chem (1997) 40: 3497-3500 [PMID:9357514]
ChEMBL Displacement of [3H]5-HT binding to cloned human 5-hydroxytryptamine 1D receptor stably expressed in CHO cells B 9.05 pIC50 0.9 nM IC50 J Med Chem (1999) 42: 4981-5001 [PMID:10585208]
ChEMBL Agonist induced [35S]GTP-gamma-S, binding in CHO cells expressing 5-HT 1d receptor F 8.96 pEC50 1.1 nM EC50 J Med Chem (1998) 41: 2667-2670 [PMID:9667955]
ChEMBL Measurement of agonist induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with 5-hydroxytryptamine 1D receptor. F 8.96 pEC50 1.1 nM EC50 J Med Chem (1997) 40: 3497-3500 [PMID:9357514]
ChEMBL Agonist-induced [35S]- GTPgammaS binding in CHO cells stably transfected with 5-hydroxytryptamine 1D receptor B 9.1 pEC50 0.8 nM EC50 J Med Chem (1999) 42: 4981-5001 [PMID:10585208]
5-ht1e receptor/5-hydroxytryptamine receptor 1E in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2182] [GtoPdb: 4] [UniProtKB: P28566]
ChEMBL Compound was tested for the displacement of [3H]5-HT binding to cloned human 5-hydroxytryptamine 1E receptor stably expressed in CHO cells B 5 pIC50 >10000 nM IC50 J Med Chem (1999) 42: 4981-5001 [PMID:10585208]
5-HT1F receptor/5-hydroxytryptamine receptor 1F in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1805] [GtoPdb: 5] [UniProtKB: P30939]
ChEMBL Compound was tested for the displacement of [3H]5-HT binding to cloned human 5-hydroxytryptamine 1F receptor stably expressed in CHO cells B 5 pIC50 >10000 nM IC50 J Med Chem (1999) 42: 4981-5001 [PMID:10585208]
5-HT2A receptor/5-hydroxytryptamine receptor 2A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL Compound was tested for the displacement of [3H]5-HT binding to cloned human 5-hydroxytryptamine 2A receptor stably expressed in CHO cells B 5.96 pIC50 1100 nM IC50 J Med Chem (1999) 42: 4981-5001 [PMID:10585208]
5-HT5A receptor/5-hydroxytryptamine receptor 5A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898]
ChEMBL Compound was tested for the displacement of [3H]5-HT binding to cloned human 5-hydroxytryptamine 5A receptor stably expressed in CHO cells B 5 pIC50 >10000 nM IC50 J Med Chem (1999) 42: 4981-5001 [PMID:10585208]
5-HT6 receptor/5-hydroxytryptamine receptor 6 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3372] [GtoPdb: 11] [UniProtKB: P31388]
ChEMBL Compound was tested for the displacement of [3H]5-HT binding to cloned rat 5-hydroxytryptamine 6 receptor stably expressed in CHO cells B 5 pIC50 >10000 nM IC50 J Med Chem (1999) 42: 4981-5001 [PMID:10585208]
5-HT7 receptor/5-hydroxytryptamine receptor 7 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3223] [GtoPdb: 12] [UniProtKB: P32305]
ChEMBL Compound was tested for the displacement of [3H]5-HT binding to cloned rat 5-hydroxytryptamine 7 receptor stably expressed in CHO cells B 6.27 pIC50 540 nM IC50 J Med Chem (1999) 42: 4981-5001 [PMID:10585208]

ChEMBL data shown on this page come from version 36:

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]