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Assay Detail

CHEMBL4303093

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

Binding
Displacement of [3H]-DTG from the Sigma2 receptor
7
Total Activities
6
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

A SARS-CoV-2 protein interaction map reveals targets for drug repurposing
David E Gordon, Gwendolyn M Jang, Mehdi Bouhaddou, Jiewei Xu, Kirsten Obernier, Kris M White, Matthew J O'Meara, Veronica V Rezelj, Jeffrey Z Guo, Danielle L Swaney, et al
Nature (2020)
PubMed 32353859 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 6.95 8.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL53325 1 8.60
CHEMBL1626 CLEMASTINE 4.0 1 7.60
CHEMBL296419 ASTEMIZOLE 4.0 2 7.02
CHEMBL76 CHLOROQUINE 4.0 1 6.30
CHEMBL4088272 1 6.10
CHEMBL1535 HYDROXYCHLOROQUINE 4.0 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL53325 Ki = 2.512 nM 8.60
CHEMBL1626 CLEMASTINE Ki = 25.12 nM 7.60
CHEMBL296419 ASTEMIZOLE Ki = 95.0 nM 7.02
CHEMBL296419 ASTEMIZOLE Ki = 95.5 nM 7.02
CHEMBL76 CHLOROQUINE Ki = 501.19 nM 6.30
CHEMBL4088272 Ki = 794.33 nM 6.10
CHEMBL1535 HYDROXYCHLOROQUINE Ki = 1000.0 nM 6.00