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Assay Detail

CHEMBL4234579

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

Binding
Inhibition of human CaV3.2 expressed in HEK293 cells assessed as suppression of T-current amplitude after 10 mins by whole cell patch clamp method
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Design and synthesis of novel anti-hyperalgesic agents based on 6-prenylnaringenin as the T-type calcium channel blockers.
Du Nguyen H, Okada T, Kitamura S, Yamaoka S, Horaguchi Y, Kasanami Y, Sekiguchi F, Tsubota M, Yoshida S, Nishikawa H, Kawabata A, Toyooka N.
Bioorg Med Chem (2018) 26 : 4410 -4427
PubMed 30031654 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.18 6.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4248823 1 6.58
CHEMBL4249364 1 6.41
CHEMBL4238346 1 6.34
CHEMBL4251381 1 6.32
CHEMBL4240812 1 6.30
CHEMBL4245811 1 6.19
CHEMBL243148 SOPHORAFLAVANONE G 1 6.00
CHEMBL376915 1 6.00
CHEMBL1537093 1 6.00
CHEMBL4242828 1 5.99
CHEMBL4237637 1 5.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4248823 IC50 = 260.0 nM 6.58
CHEMBL4249364 IC50 = 390.0 nM 6.41
CHEMBL4238346 IC50 = 460.0 nM 6.34
CHEMBL4251381 IC50 = 480.0 nM 6.32
CHEMBL4240812 IC50 = 500.0 nM 6.30
CHEMBL4245811 IC50 = 640.0 nM 6.19
CHEMBL243148 SOPHORAFLAVANONE G IC50 = 1000.0 nM 6.00
CHEMBL376915 IC50 = 1000.0 nM 6.00
CHEMBL1537093 IC50 = 1000.0 nM 6.00
CHEMBL4242828 IC50 = 1020.0 nM 5.99
CHEMBL4237637 IC50 = 1250.0 nM 5.90