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Assay Detail

CHEMBL4390736

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

Binding
Displacement [3H]-DTG from sigma 2 receptor (unknown origin) expressed in HEK cell membranes
42
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sigma intracellular receptor 2 (CHEMBL4105907)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

SYA 013 analogs as moderately selective sigma-2 (σ2) ligands: Structure-affinity relationship studies.
Al-Ghanim L, Zhu XY, Asong G, Ablordeppey SY.
Bioorg Med Chem (2019) 27 : 2421 -2426
PubMed 30737135 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 42 7.81 8.67

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3321792 2 8.67
CHEMBL4577233 2 8.66
CHEMBL4446729 2 8.60
CHEMBL476108 2 8.29
CHEMBL1940412 1 8.29
CHEMBL1946126 2 8.23
CHEMBL4574793 2 8.10
CHEMBL3321791 2 8.09
CHEMBL4573441 2 8.08
CHEMBL1946253 2 8.07
CHEMBL4581305 1 7.88
CHEMBL3321789 2 7.75
CHEMBL3321788 2 7.60
CHEMBL4554850 2 7.60
CHEMBL1940414 1 7.60
CHEMBL3321790 2 7.54
CHEMBL4533305 2 7.50
CHEMBL1940413 2 7.48
CHEMBL4516724 2 7.40
CHEMBL4462108 2 7.37
CHEMBL340211 AZAPERONE 2.0 2 7.30
CHEMBL1940408 1 7.29
CHEMBL3289383 2 6.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3321792 Ki = 2.138 nM 8.67
CHEMBL3321792 Ki = 2.2 nM 8.66
CHEMBL4577233 Ki = 2.2 nM 8.66
CHEMBL4577233 Ki = 2.239 nM 8.65
CHEMBL4446729 Ki = 2.512 nM 8.60
CHEMBL4446729 Ki = 2.7 nM 8.57
CHEMBL476108 Ki = 5.129 nM 8.29
CHEMBL1940412 Ki = 5.12 nM 8.29
CHEMBL476108 Ki = 5.6 nM 8.25
CHEMBL1946126 Ki = 5.9 nM 8.23
CHEMBL1946126 Ki = 5.888 nM 8.23
CHEMBL4574793 Ki = 7.943 nM 8.10
CHEMBL4574793 Ki = 8.0 nM 8.10
CHEMBL3321791 Ki = 8.1 nM 8.09
CHEMBL3321791 Ki = 8.128 nM 8.09
CHEMBL4573441 Ki = 8.4 nM 8.08
CHEMBL4573441 Ki = 8.511 nM 8.07
CHEMBL1946253 Ki = 8.511 nM 8.07
CHEMBL1946253 Ki = 8.5 nM 8.07
CHEMBL4581305 Ki = 13.1 nM 7.88
CHEMBL3321789 Ki = 18.0 nM 7.75
CHEMBL3321789 Ki = 19.95 nM 7.70
CHEMBL3321788 Ki = 25.12 nM 7.60
CHEMBL4554850 Ki = 25.12 nM 7.60
CHEMBL1940414 Ki = 25.1 nM 7.60
CHEMBL4554850 Ki = 26.0 nM 7.58
CHEMBL3321788 Ki = 27.0 nM 7.57
CHEMBL3321790 Ki = 29.0 nM 7.54
CHEMBL3321790 Ki = 29.51 nM 7.53
CHEMBL4533305 Ki = 32.0 nM 7.50
CHEMBL4533305 Ki = 32.36 nM 7.49
CHEMBL1940413 Ki = 33.11 nM 7.48
CHEMBL1940413 Ki = 33.0 nM 7.48
CHEMBL4516724 Ki = 39.81 nM 7.40
CHEMBL4462108 Ki = 43.0 nM 7.37
CHEMBL4462108 Ki = 42.66 nM 7.37
CHEMBL4516724 Ki = 44.0 nM 7.36
CHEMBL340211 AZAPERONE Ki = 50.12 nM 7.30
CHEMBL1940408 Ki = 51.5 nM 7.29
CHEMBL340211 AZAPERONE Ki = 52.0 nM 7.28
CHEMBL3289383 Ki = 600.0 nM 6.22
CHEMBL3289383 Ki = 630.96 nM 6.20