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| ChEMBL ligand: CHEMBL4576388 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| NTS1 receptor/Neurotensin receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4123] [GtoPdb: 309] [UniProtKB: P30989] | ||||||||
| ChEMBL | Allosteric modulation of human GFP-fused PK-tagged Gq-coupled NTR1 expressed in CHOK1 cells assessed as induction of NT (8 to 13) peptide-mediated beta-arrestin recruitment measured after 90 mins by pathhunter assay | B | 6.47 | pEC50 | 340 | nM | EC50 | J Med Chem (2019) 62: 8357-8363 [PMID:31390201] |
| ChEMBL | Positive allosteric modulation of recombinant human NTR1 expressed in HEK293 cells assessed as increase in [125I]-neurotensin binding measured after 45 mins | B | 6.85 | pEC50 | 140 | nM | EC50 | J Med Chem (2019) 62: 8357-8363 [PMID:31390201] |
| ChEMBL | Positive allosteric modulation of human GFP-fused PK-tagged Gq-coupled NTR1 expressed in CHOK1 cells assessed as effect on NT (8 to 13) peptide-mediated calcium flux by measuring neurotensin EC50 at 0.0088 to 2.15 uM (Rvb = 0.035 nM) | F | 8.93 | pEC50 | 1.18 | nM | EC50 | J Med Chem (2019) 62: 8357-8363 [PMID:31390201] |
ChEMBL data shown on this page come from version 35:
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]