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ChEMBL ligand: CHEMBL444832 (PD-157672) |
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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 | 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]