L-733,060 [Ligand Id: 13432] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL27006 (L-733060) |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
| 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] | ||||||||
| GtoPdb | Determined as antagonism of substande P-induced calcium mobilisation in CHO cells expressing hTACR1 | - | 9.1 | pKi | 0.8 | nM | Ki | Eur J Pharmacol (1996) 317: 129-35 [PMID:8982729] |
| ChEMBL | Binding affinity towards Neurokinin -1(NK-1) receptor of human by using [125I]- Tyr8 substance P as a radioligand in CHO cells | B | 9 | pIC50 | 1 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 1345-1350 |
| ChEMBL | Binding affinity at human tachykinin receptor 1 by measuring its ability to displace [125I]-labeled substance P from the cloned receptor expressed in CHO cells. | B | 9 | pIC50 | 1 | nM | IC50 | J Med Chem (1998) 41: 4623-4635 [PMID:9804702] |
| ChEMBL | Compound was tested for the displacement of [ 1251] Substance P from hNK1 receptor in CHO cells | B | 9 | pIC50 | 1 | nM | IC50 | Bioorg Med Chem Lett (1994) 4: 2545-2550 |
| ChEMBL | Binding affinity for human NK1 receptor expressed in CHO cells | B | 9 | pIC50 | 1 | nM | IC50 | Bioorg Med Chem Lett (1994) 4: 2733-2734 |
| ChEMBL | Binding affinity was measured against the Tachykinin receptor 1 in CHO-expressed hNK1 using [125I]SP. | B | 9 | pIC50 | 1 | nM | IC50 | J Med Chem (1998) 41: 3609-3623 [PMID:9733486] |
| ChEMBL | Antagonist activity at NK1 receptor (unknown origin) | B | 9 | pIC50 | 1 | nM | IC50 | Bioorg Med Chem (2013) 21: 6264-6273 [PMID:24075145] |
| ChEMBL | Ability to displace [125I]-substance P from hNK1 receptor in chinese hamster ovarian (CHO) cells | B | 9 | pIC50 | 1 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 1845-1850 [PMID:9873445] |
| ChEMBL | Displacement of [125I]- Substance P from human Neurokinin 1 (hNK1) receptor expressed in CHO cells | B | 9.06 | pIC50 | 0.87 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 209-212 |
| ChEMBL | Displacement of [125I]-labeled SP from human Tachykinin receptor 1 expressed in CHO cells | B | 9.06 | pIC50 | 0.87 | nM | IC50 | J Med Chem (1996) 39: 1760-1762 [PMID:8627597] |
| ChEMBL | Displacement of [125I]-labeled SP from human NK-1 receptor expressed in CHO cells | B | 9.06 | pIC50 | 0.87 | nM | IC50 | J Med Chem (2021) 64: 9786-9874 [PMID:34213340] |
| NK1 receptor/Neurokinin 1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4027] [GtoPdb: 360] [UniProtKB: P14600] | ||||||||
| ChEMBL | Antagonism of NK1 receptor in rat liver microsomes. | F | 9.1 | pIC50 | 0.8 | nM | IC50 | Bioorg Med Chem Lett (1997) 7: 2959-2962 |
| NK2 receptor/Neurokinin 2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2327] [GtoPdb: 361] [UniProtKB: P21452] | ||||||||
| ChEMBL | Tested for inhibition of human Neurokinin Tachykinin receptor 2. | B | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 209-212 |
| NK3 receptor/Neurokinin 3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4429] [GtoPdb: 362] [UniProtKB: P29371] | ||||||||
| ChEMBL | Tested for inhibition of human Tachykinin receptor 3 | B | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 209-212 |
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]
