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