N',2-diphenylquinoline-4-carbohydrazide 8m [Ligand Id: 2130] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL221445
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  • NK1 receptor/Neurokinin 1 receptor in Human [ChEMBL: CHEMBL249] [GtoPdb: 360] [UniProtKB: P25103]
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  • NK2 receptor/Neurokinin 2 receptor in Human [ChEMBL: CHEMBL2327] [GtoPdb: 361] [UniProtKB: P21452]
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  • NK3 receptor/Neurokinin 3 receptor in Human [ChEMBL: CHEMBL4429] [GtoPdb: 362] [UniProtKB: P29371]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809]
ChEMBL Displacement of labeled MK499 from cloned hERG potassium channel expressed in HEK cells B 5.05 pKi >9000 nM Ki Bioorg Med Chem Lett (2006) 16: 5752-5756 [PMID:16950617]
NK1 receptor/Neurokinin 1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL249] [GtoPdb: 360] [UniProtKB: P25103]
ChEMBL Inhibition of human NK1 receptor B 6 pIC50 >1000 nM IC50 Bioorg Med Chem Lett (2006) 16: 5752-5756 [PMID:16950617]
NK2 receptor/Neurokinin 2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2327] [GtoPdb: 361] [UniProtKB: P21452]
ChEMBL Inhibition of human NK2 receptor B 7.3 pIC50 50 nM IC50 Bioorg Med Chem Lett (2006) 16: 5752-5756 [PMID:16950617]
NK3 receptor/Neurokinin 3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4429] [GtoPdb: 362] [UniProtKB: P29371]
ChEMBL Displacement of [125I]neurokinin B from human cloned NK3 receptor expressed in CHO cells B 8.4 pIC50 4 nM IC50 Bioorg Med Chem Lett (2006) 16: 5752-5756 [PMID:16950617]
GtoPdb - - 8.4 pIC50 - - - Bioorg Med Chem Lett (2006) 16: 5752-6 [PMID:16950617]
ChEMBL Antagonist activity at human NK3 receptor expressed in CHO cells assessed as inhibition of inositol phosphate generation F 8.52 pIC50 3 nM IC50 Bioorg Med Chem Lett (2006) 16: 5752-5756 [PMID:16950617]

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]