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Assay Detail

CHEMBL5339618

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 assessed as inhibition constant by competition binding assay
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Targeting σ<sub>2</sub>R/TMEM97 with novel aminotetralins.
Wood MD, Sahn JJ, Martin SF.
Eur J Med Chem (2022) 243 : 114696 -114696
PubMed 36088757 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 26 6.64 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5400163 1 7.92
CHEMBL5438672 1 7.80
CHEMBL5408937 1 7.68
CHEMBL5411467 1 7.48
CHEMBL5406262 1 7.40
CHEMBL5401174 1 7.07
CHEMBL5427018 1 6.98
CHEMBL5415235 1 6.85
CHEMBL5419308 1 6.73
CHEMBL5403404 1 6.70
CHEMBL5422903 1 6.70
CHEMBL5395472 1 6.65
CHEMBL5401938 1 6.60
CHEMBL5440859 1 6.60
CHEMBL5439530 1 6.59
CHEMBL5437307 1 6.58
CHEMBL5393862 1 6.49
CHEMBL5408800 1 6.32
CHEMBL5397633 1 6.05
CHEMBL5423845 1 6.01
CHEMBL5402989 1 5.98
CHEMBL5189158 1 5.89
CHEMBL5394787 1 5.78
CHEMBL5438518 1 5.68
CHEMBL5419932 1 5.53
CHEMBL5418564 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5400163 Ki = 12.0 nM 7.92
CHEMBL5438672 Ki = 16.0 nM 7.80
CHEMBL5408937 Ki = 21.0 nM 7.68
CHEMBL5411467 Ki = 33.0 nM 7.48
CHEMBL5406262 Ki = 40.0 nM 7.40
CHEMBL5401174 Ki = 86.0 nM 7.07
CHEMBL5427018 Ki = 104.0 nM 6.98
CHEMBL5415235 Ki = 140.0 nM 6.85
CHEMBL5419308 Ki = 187.0 nM 6.73
CHEMBL5403404 Ki = 200.0 nM 6.70
CHEMBL5422903 Ki = 199.0 nM 6.70
CHEMBL5395472 Ki = 223.0 nM 6.65
CHEMBL5401938 Ki = 251.0 nM 6.60
CHEMBL5440859 Ki = 250.0 nM 6.60
CHEMBL5439530 Ki = 254.0 nM 6.59
CHEMBL5437307 Ki = 266.0 nM 6.58
CHEMBL5393862 Ki = 321.0 nM 6.49
CHEMBL5408800 Ki = 474.0 nM 6.32
CHEMBL5397633 Ki = 887.0 nM 6.05
CHEMBL5423845 Ki = 973.0 nM 6.01
CHEMBL5402989 Ki = 1054.0 nM 5.98
CHEMBL5189158 Ki = 1279.0 nM 5.89
CHEMBL5394787 Ki = 1649.0 nM 5.78
CHEMBL5438518 Ki = 2101.0 nM 5.68
CHEMBL5419932 Ki = 2944.0 nM 5.53
CHEMBL5418564 Ki > 10000.0 nM -