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ChEMBL ligand: CHEMBL42407 (Lanepitant) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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NK1 receptor/Neurokinin 1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL249] [GtoPdb: 360] [UniProtKB: P25103] | ||||||||
ChEMBL | Inhibition of substance P induced contraction of rabbit vena ceva (RVC) tissue expressing Tachykinin receptor 1 | F | 9.4 | pKd | 0.4 | nM | Kd | J Med Chem (1996) 39: 736-748 [PMID:8576917] |
GtoPdb | - | - | 10 | pKi | 0.1 | nM | Ki | J Pharmacol Exp Ther (1995) 275: 737-44 [PMID:7473161] |
ChEMBL | In vitro inhibition of binding of [125I]Bolton-Hunter SP to Tachykinin receptor 1 in human IM-9 cell line | B | 9.64 | pIC50 | 0.23 | nM | IC50 | Bioorg Med Chem Lett (2001) 11: 1643-1646 [PMID:11425527] |
GtoPdb | - | - | 9.82 | pIC50 | 0.15 | nM | IC50 | Expert Opin Ther Pat (2010) 20: 1019-45 [PMID:20533894] |
ChEMBL | Inhibitory activity against Tachykinin receptor 1 in human IM-9 cells using [125I]-labeled Boltan-Hunter substance P as radioligand | B | 9.82 | pIC50 | 0.15 | nM | IC50 | J Med Chem (1996) 39: 736-748 [PMID:8576917] |
Neurokinin 2 receptor in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3433] [UniProtKB: P79218] | ||||||||
ChEMBL | Inhibition of neurokinin A induced contraction of rabbit pulmonary artery (RPA) tissue expressing Tachykinin receptor 2 | F | 4.7 | pKd | 19952.62 | nM | Kd | J Med Chem (1996) 39: 736-748 [PMID:8576917] |
NK3 receptor/Neurokinin 3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3154] [GtoPdb: 362] [UniProtKB: P16177] | ||||||||
ChEMBL | Inhibition of neurokinin B induced contraction of rat portal vein (RPV) tissue expressing Tachykinin receptor 3 | F | 4.7 | pKd | 19952.62 | nM | Kd | J Med Chem (1996) 39: 736-748 [PMID:8576917] |
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]