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 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]