ZD6021 [Ligand Id: 2109] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL129683 (ZD-6021)
  • 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
NK1 receptor/Neurokinin 1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL249] [GtoPdb: 360] [UniProtKB: P25103]
ChEMBL Inhibition of binding of [3H]SP to Tachykinin receptor 1 of human tachykinin receptor expressed in mouse erythroleukemia cells B 9.92 pKi 0.12 nM Ki J Med Chem (2002) 45: 3972-3983 [PMID:12190319]
ChEMBL Binding affinity against human cloned Tachykinin receptor 1 expressed in MEL cells B 10 pKi 0.1 nM Ki Bioorg Med Chem Lett (2001) 11: 2769-2773 [PMID:11591520]
GtoPdb - - 9.9 pIC50 - - - J Pharmacol Exp Ther (2001) 298: 307-15 [PMID:11408556]
NK2 receptor/Neurokinin 2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2327] [GtoPdb: 361] [UniProtKB: P21452]
ChEMBL Inhibition of binding of [3H]NKA to human Tachykinin receptor 2 (NK2) expressed in mouse erythroleukemia cells B 9.19 pKi 0.64 nM Ki J Med Chem (2002) 45: 3972-3983 [PMID:12190319]
ChEMBL Binding affinity against human cloned Tachykinin receptor 2 expressed in MEL cells B 9.22 pKi 0.6 nM Ki Bioorg Med Chem Lett (2001) 11: 2769-2773 [PMID:11591520]
NK3 receptor/Neurokinin 3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4429] [GtoPdb: 362] [UniProtKB: P29371]
ChEMBL Binding affinity against human cloned Tachykinin receptor 3 expressed in MEL cells B 7.13 pKi 74 nM Ki Bioorg Med Chem Lett (2001) 11: 2769-2773 [PMID:11591520]
ChEMBL Inhibition of binding of [125I]MPNI to human Tachykinin receptor 3 (NK3) expressed in mouse erythroleukemia cells B 7.13 pKi 74 nM Ki J Med Chem (2002) 45: 3972-3983 [PMID:12190319]

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]