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Assay Detail

CHEMBL5168664

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

Binding
Inhibition of human alpha1c/beta2a/alpha2delta1 Cav1.2 expressed in HEK293 cells assessed as Ca2+ current at -80 mV holding potential by patch clamp technique
2
Total Activities
2
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

L-type calcium channel alpha-1c/beta-2/alpha2delta-1 (CHEMBL4106164)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Structural Modifications of Nimodipine Lead to Novel PDE1 Inhibitors with Anti-pulmonary Fibrosis Effects.
Huang MX, Tian YJ, Han C, Liu RD, Xie X, Yuan Y, Yang YY, Li Z, Chen J, Luo HB, Wu Y.
J Med Chem (2022) 65 : 8444 -8455
PubMed 35666471 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.53 7.53
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1428 NIMODIPINE 4.0 1 7.53
CHEMBL5180169 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1428 NIMODIPINE IC50 = 29.8 nM 7.53
CHEMBL5180169 Inhibition - % -