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Assay Detail

CHEMBL785241

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

Functional
In vitro inhibition of K+ induced contractions of the isolated rat aorta.
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Aorta
Confidence 9 — Direct single protein target
Curated By Expert

Target

Voltage-dependent L-type calcium channel subunit alpha-1C (CHEMBL3762)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Novel calcium antagonists with both calcium overload inhibition and antioxidant activity. 1. 2-(3, 5-di-tert-butyl-4-hydroxyphenyl)-3-(aminopropyl)thiazolidinones.
Kato T, Ozaki T, Tamura K, Suzuki Y, Akima M, Ohi N.
J Med Chem (1998) 41 : 4309 -4316
PubMed 9784106 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 6.36 7.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL107949 1 7.21
CHEMBL137151 1 7.03
CHEMBL23 DILTIAZEM 4.0 1 7.00
CHEMBL138800 1 6.92
CHEMBL423535 1 6.75
CHEMBL344472 1 6.70
CHEMBL335343 1 6.68
CHEMBL137172 1 6.64
CHEMBL137094 1 6.64
CHEMBL336705 1 6.60
CHEMBL137352 1 6.52
CHEMBL344252 1 6.38
CHEMBL137324 1 6.37
CHEMBL137436 1 6.22
CHEMBL137009 1 6.12
CHEMBL341710 1 6.08
CHEMBL137390 1 5.92
CHEMBL136357 1 5.82
CHEMBL138484 1 5.77
CHEMBL137514 1 5.62
CHEMBL138126 1 5.48
CHEMBL137426 1 5.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL107949 IC50 = 62.0 nM 7.21
CHEMBL137151 IC50 = 93.0 nM 7.03
CHEMBL23 DILTIAZEM IC50 = 100.0 nM 7.00
CHEMBL138800 IC50 = 120.0 nM 6.92
CHEMBL423535 IC50 = 180.0 nM 6.75
CHEMBL344472 IC50 = 200.0 nM 6.70
CHEMBL335343 IC50 = 210.0 nM 6.68
CHEMBL137172 IC50 = 230.0 nM 6.64
CHEMBL137094 IC50 = 230.0 nM 6.64
CHEMBL336705 IC50 = 250.0 nM 6.60
CHEMBL137352 IC50 = 300.0 nM 6.52
CHEMBL344252 IC50 = 420.0 nM 6.38
CHEMBL137324 IC50 = 430.0 nM 6.37
CHEMBL137436 IC50 = 600.0 nM 6.22
CHEMBL137009 IC50 = 760.0 nM 6.12
CHEMBL341710 IC50 = 840.0 nM 6.08
CHEMBL137390 IC50 = 1200.0 nM 5.92
CHEMBL136357 IC50 = 1500.0 nM 5.82
CHEMBL138484 IC50 = 1700.0 nM 5.77
CHEMBL137514 IC50 = 2400.0 nM 5.62
CHEMBL138126 IC50 = 3300.0 nM 5.48
CHEMBL137426 IC50 = 4400.0 nM 5.36