PD157672 [Ligand Id: 2125] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL444832 (PD-157672)
  • NK1 receptor/Neurokinin 1 receptor in Human [ChEMBL: CHEMBL249] [GtoPdb: 360] [UniProtKB: P25103]
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  • NK3 receptor/Neurokinin 3 receptor in Human [ChEMBL: CHEMBL4429] [GtoPdb: 362] [UniProtKB: P29371]
  • NK3 receptor/Neurokinin 3 receptor in Rat [ChEMBL: CHEMBL3154] [GtoPdb: 362] [UniProtKB: P16177]
  • Neurokinin 3 receptor in Guinea pig [ChEMBL: CHEMBL3799] [UniProtKB: P30098]
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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 Inhibitory activity against Tachykinin receptor 1 in human lymphoma IM9 cells labeled with [125 I] Bolton-Hunter substance P B 5 pIC50 >10000 nM IC50 J Med Chem (1996) 39: 1664-1675 [PMID:8648606]
ChEMBL Binding affinity for NK1 receptor binding sites in human lymphoma IM9 cells by using [125I]-Bolton-Hunter substance P as radioligand B 5 pIC50 10000 nM IC50 Bioorg Med Chem Lett (1994) 4: 1679-1684
Neurokinin 2 receptor in Hamster (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2304405] [UniProtKB: P51144]
ChEMBL Inhibitory activity against Tachykinin receptor 2 in membranes prepared from hamster urinary bladder labeled with [125 I] NKA B 5.18 pIC50 6540 nM IC50 J Med Chem (1996) 39: 1664-1675 [PMID:8648606]
ChEMBL Binding affinity for NK2 receptor binding sites in membranes prepared from hamster urinary bladder by using [125I]NKA as radioligand B 5.18 pIC50 6540 nM IC50 Bioorg Med Chem Lett (1994) 4: 1679-1684
NK3 receptor/Neurokinin 3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4429] [GtoPdb: 362] [UniProtKB: P29371]
GtoPdb - - 8 pKi - - - Mol Pharmacol (1995) 48: 711-6 [PMID:7476898]
ChEMBL Binding affinity towards human Tachykinin receptor 3 stably expressed in CHO cells using [125I][MePhe7]-NKB as radioligand B 7.4 pIC50 40 nM IC50 Bioorg Med Chem Lett (1995) 5: 1773-1778
ChEMBL Inhibitory activity against cloned human Tachykinin receptor 3 in CHO cells labeled with [125I][MePhe7]-NKB B 7.8 pIC50 16 nM IC50 J Med Chem (1996) 39: 1664-1675 [PMID:8648606]
ChEMBL Compound was tested for binding affinity against human Tachykinin receptor 3 in CHO cells B 7.8 pIC50 16 nM IC50 Bioorg Med Chem Lett (1995) 5: 1773-1778
ChEMBL Displacement of [125I][MePhe]-NKB from human NK3 receptor expressed in CHO cells B 7.8 pIC50 16 nM IC50 Bioorg Med Chem Lett (1994) 4: 1679-1684
GtoPdb - - 7.9 pIC50 12.1 nM IC50 J Biol Chem (1996) 271: 20250-7 [PMID:8702757];
J Med Chem (1996) 39: 1664-75 [PMID:8648606]
NK3 receptor/Neurokinin 3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3154] [GtoPdb: 362] [UniProtKB: P16177]
ChEMBL Inhibitory activity against cloned human Tachykinin receptor 3 in CHO cells labeled with [125I][MePhe7]-NKB B 5.76 pIC50 1730 nM IC50 J Med Chem (1996) 39: 1664-1675 [PMID:8648606]
Neurokinin 3 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3799] [UniProtKB: P30098]
ChEMBL Inhibitory activity against Tachykinin receptor 3 in guinea pig cortical membranes labeled with [125 I]-[MePhe7] B 8.05 pIC50 9 nM IC50 J Med Chem (1996) 39: 1664-1675 [PMID:8648606]
ChEMBL Binding affinity for NK3 receptor binding sites in guinea pig cortical membranes by using [125I][MePhe7]-NKB as radioligand B 8.05 pIC50 9 nM IC50 Bioorg Med Chem Lett (1994) 4: 1679-1684

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]