BD-1063 [Ligand Id: 12125] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL73824
  • GluN2B/Glutamate [NMDA] receptor subunit epsilon 2 in Mouse [ChEMBL: CHEMBL3442] [GtoPdb: 457] [UniProtKB: Q01097]
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  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Rat [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
GluN2B/Glutamate [NMDA] receptor subunit epsilon 2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3442] [GtoPdb: 457] [UniProtKB: Q01097]
ChEMBL Displacement of [3H]ifenprodil from GluN2B in mouse LTK cells assessed as inhibition constant measured after 120 mins by scintillation counting method B 7.31 pKi 49 nM Ki J Med Chem (2023) 66: 4999-5020 [PMID:36946301]
Sigma-1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4153] [UniProtKB: Q60492]
ChEMBL Displacement of [3H]-(+)-pentazocine from guinea pig brain membrane sigma 1 receptor assessed as inhibition constant measured after 120 mins by scintillation counting method B 6.35 pKi 449 nM Ki J Med Chem (2023) 66: 4999-5020 [PMID:36946301]
ChEMBL Displacement of [3H]-(+)-pentazocine from Dunkin-Hartley guinea pig brain cortex Sigma 1 receptor incubated for 150 mins by liquid scintillation counting analysis B 7.85 pKi 14 nM Ki Eur J Med Chem (2022) 230: 114091-114091 [PMID:35016113]
σ2/Sigma intracellular receptor 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105864] [GtoPdb: 2553] [UniProtKB: Q5U3Y7]
ChEMBL Displacement of [3H]-DTG from Sprague-Dawley rat liver Sigma 2 receptor incubated for 120 mins in presence of [3H]-(+)-pentazocine by liquid scintillation counting analysis B 6.69 pKi 204 nM Ki Eur J Med Chem (2022) 230: 114091-114091 [PMID:35016113]
ChEMBL Displacement of [3H]-(+)-DTG from rat liver homogenate S2R incubated for 120 mins by liquid scintillation counting method B 6.69 pKi 204 nM Ki J Med Chem (2023) 66: 11447-11463 [PMID:37535861]
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
ChEMBL Ability to displace [3H](+)-pentazocine at sigma receptor in guinea pig brain membrane was determined B 8.04 pKi 9.2 nM Ki J Med Chem (1993) 36: 2311-2320 [PMID:8360875]
GtoPdb Displacement of [3H](+)pentazocine from human sigma 1 receptor expressed in HEK293 cells, in a membrane radiologand binding assay - 8.2 pKi 6.3 nM Ki J Med Chem (2012) 55: 8211-24 [PMID:22784008]
ChEMBL Displacement of [3H](+)pentazocine from human sigma 1 receptor transfected in HEK293 cell membranes after 120 mins by scintillation counter B 8.2 pKi 6.3 nM Ki J Med Chem (2012) 55: 8211-8224 [PMID:22784008]
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9]
ChEMBL Displacement of [3H]-(+)-pentazocine from rat liver homogenate S1R incubated for 120 mins by liquid scintillation counting method B 7.85 pKi 14 nM Ki J Med Chem (2023) 66: 11447-11463 [PMID:37535861]

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]