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Assay Detail

CHEMBL1174684

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membrane
ChEMBL ↗
118
Total Activities
60
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Brain
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sigma non-opioid intracellular receptor 1 (CHEMBL4153) ↗
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

5D-QSAR for spirocyclic sigma1 receptor ligands by Quasar receptor surface modeling.
Oberdorf C, Schmidt TJ, Wünsch B.
Eur J Med Chem (2010) 45 : 3116 -3124
PubMed 20427100 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 118 7.87 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1169953 — — 2 9.52
CHEMBL1169950 — — 2 9.49
CHEMBL1171555 — — 2 9.37
CHEMBL1171554 — — 2 9.37
CHEMBL1172688 — — 2 9.31
CHEMBL1172689 — — 2 9.31
CHEMBL1170982 — — 2 9.18
CHEMBL1170963 — — 2 9.18
CHEMBL1170964 — — 2 9.18
CHEMBL1170546 — — 2 9.09
CHEMBL1170545 — — 2 9.09
CHEMBL1170968 — — 2 9.00
CHEMBL1171781 — — 2 8.96
CHEMBL1171905 — — 2 8.96
CHEMBL1172290 — — 2 8.89
CHEMBL1171689 — — 2 8.89
CHEMBL1169777 — — 2 8.82
CHEMBL1172291 — — 2 8.82
CHEMBL1170547 — — 2 8.66
CHEMBL1171726 — — 2 8.64
CHEMBL1169778 — — 2 8.64
CHEMBL1170334 — — 2 8.59
CHEMBL1171872 — — 2 8.59
CHEMBL1171418 — — 2 8.49
CHEMBL1171419 — — 2 8.49
CHEMBL1171232 — — 2 8.48
CHEMBL1169779 — — 2 8.44
CHEMBL1170773 — — 2 8.27
CHEMBL1170965 — — 2 8.24
CHEMBL1169951 — — 2 8.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1169953 — Ki = 0.3 nM 9.52
CHEMBL1169953 — Ki = 0.3 nM 9.52
CHEMBL1169950 — Ki = 0.32 nM 9.49
CHEMBL1169950 — Ki = 0.32 nM 9.49
CHEMBL1171555 — Ki = 0.43 nM 9.37
CHEMBL1171554 — Ki = 0.43 nM 9.37
CHEMBL1172689 — Ki = 0.49 nM 9.31
CHEMBL1172688 — Ki = 0.49 nM 9.31
CHEMBL1170963 — Ki = 0.66 nM 9.18
CHEMBL1170964 — Ki = 0.66 nM 9.18
CHEMBL1170982 — Ki = 0.66 nM 9.18
CHEMBL1170546 — Ki = 0.81 nM 9.09
CHEMBL1170545 — Ki = 0.81 nM 9.09
CHEMBL1170968 — Ki = 1.0 nM 9.00
CHEMBL1170968 — Ki = 1.0 nM 9.00
CHEMBL1171905 — Ki = 1.1 nM 8.96
CHEMBL1171781 — Ki = 1.1 nM 8.96
CHEMBL1172290 — Ki = 1.3 nM 8.89
CHEMBL1171689 — Ki = 1.3 nM 8.89
CHEMBL1169777 — Ki = 1.5 nM 8.82
CHEMBL1172291 — Ki = 1.5 nM 8.82
CHEMBL1172290 — Ki = 1.5 nM 8.82
CHEMBL1172689 — Ki = 1.5 nM 8.82
CHEMBL1170547 — Ki = 2.2 nM 8.66
CHEMBL1170546 — Ki = 2.2 nM 8.66
CHEMBL1169778 — Ki = 2.3 nM 8.64
CHEMBL1171726 — Ki = 2.3 nM 8.64
CHEMBL1170334 — Ki = 2.6 nM 8.59
CHEMBL1171872 — Ki = 2.6 nM 8.59
CHEMBL1171418 — Ki = 3.2 nM 8.49
CHEMBL1171419 — Ki = 3.2 nM 8.49
CHEMBL1171232 — Ki = 3.3 nM 8.48
CHEMBL1171418 — Ki = 3.3 nM 8.48
CHEMBL1169779 — Ki = 3.6 nM 8.44
CHEMBL1169778 — Ki = 3.6 nM 8.44
CHEMBL1171781 — Ki = 3.7 nM 8.43
CHEMBL1171232 — Ki = 3.7 nM 8.43
CHEMBL1170773 — Ki = 5.4 nM 8.27
CHEMBL1170982 — Ki = 5.4 nM 8.27
CHEMBL1170964 — Ki = 5.8 nM 8.24
CHEMBL1170965 — Ki = 5.8 nM 8.24
CHEMBL1169951 — Ki = 5.9 nM 8.23
CHEMBL1169951 — Ki = 5.9 nM 8.23
CHEMBL1169777 — Ki = 6.3 nM 8.20
CHEMBL1170769 — Ki = 6.3 nM 8.20
CHEMBL1170547 — Ki = 7.3 nM 8.14
CHEMBL1171727 — Ki = 7.3 nM 8.14
CHEMBL1169952 — Ki = 7.7 nM 8.11
CHEMBL1169952 — Ki = 7.7 nM 8.11
CHEMBL513470 — Ki = 7.7 nM 8.11