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Assay Detail

CHEMBL809529

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

Binding
Binding affinity at Sigma receptor type 2 on rat liver membranes receptor by [3H]DTG displacement.
21
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Liver
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Expert

Target

Sigma non-opioid intracellular receptor 1 (CHEMBL3602)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and sigma binding properties of 2'-substituted 5,9 alpha-dimethyl-6,7-benzomorphans.
Danso-Danquah R, Bai X, Zhang X, Mascarella SW, Williams W, Sine B, Bowen WD, Carroll FI.
J Med Chem (1995) 38 : 2978 -2985
PubMed 7636860 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 6.49 7.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL560 1 7.44
CHEMBL101300 2 7.37
CHEMBL103157 2 7.29
CHEMBL103156 1 7.25
CHEMBL318877 2 6.72
CHEMBL101607 2 6.64
CHEMBL103816 1 6.59
CHEMBL330601 1 6.53
CHEMBL276078 2 6.42
CHEMBL99854 1 6.30
CHEMBL103319 1 6.16
CHEMBL102406 1 6.08
CHEMBL60542 (+)-PENTAZOCINE 1 5.81
CHEMBL317354 1 5.72
CHEMBL100789 1 5.69
CHEMBL274099 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL560 Ki = 36.5 nM 7.44
CHEMBL101300 Ki = 43.0 nM 7.37
CHEMBL103157 Ki = 51.8 nM 7.29
CHEMBL103156 Ki = 56.4 nM 7.25
CHEMBL103157 Ki = 154.0 nM 6.81
CHEMBL318877 Ki = 192.0 nM 6.72
CHEMBL101607 Ki = 230.0 nM 6.64
CHEMBL103816 Ki = 258.0 nM 6.59
CHEMBL101300 Ki = 264.0 nM 6.58
CHEMBL330601 Ki = 295.0 nM 6.53
CHEMBL276078 Ki = 381.0 nM 6.42
CHEMBL276078 Ki = 429.0 nM 6.37
CHEMBL101607 Ki = 487.0 nM 6.31
CHEMBL99854 Ki = 501.0 nM 6.30
CHEMBL103319 Ki = 691.0 nM 6.16
CHEMBL102406 Ki = 832.0 nM 6.08
CHEMBL60542 (+)-PENTAZOCINE Ki = 1540.0 nM 5.81
CHEMBL318877 Ki = 1710.0 nM 5.77
CHEMBL317354 Ki = 1900.0 nM 5.72
CHEMBL100789 Ki = 2037.0 nM 5.69
CHEMBL274099 Ki > 10000.0 nM -