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Assay Detail

CHEMBL772315

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

Functional
Vasorelaxant potency in isolated potassium (K(+)-depolarized rabbit thoracic aorta.
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Oryctolagus cuniculus
Tissue Thoracic aorta
Confidence 1 — Organism
Curated By Expert

Target

Oryctolagus cuniculus (CHEMBL374)
Type ORGANISM
Organism Oryctolagus cuniculus

Publication

Dihydropyrimidine calcium channel blockers: 2-heterosubstituted 4-aryl-1,4-dihydro-6-methyl-5-pyrimidinecarboxylic acid esters as potent mimics of dihydropyridines.
Atwal KS, Rovnyak GC, Schwartz J, Moreland S, Hedberg A, Gougoutas JZ, Malley MF, Floyd DM.
J Med Chem (1990) 33 : 1510 -1515
PubMed 2329573 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 7.09 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL475534 NITRENDIPINE 3.0 1 9.00
CHEMBL3392282 1 8.40
CHEMBL3392286 1 8.22
CHEMBL2398396 1 8.15
CHEMBL3392281 1 8.05
CHEMBL3392283 1 7.80
CHEMBL3392280 1 7.58
CHEMBL3392284 1 7.52
CHEMBL3392285 1 7.44
CHEMBL39925 1 6.89
CHEMBL3392289 1 6.77
CHEMBL472962 1 6.75
CHEMBL515270 1 6.72
CHEMBL282279 1 6.55
CHEMBL3392279 1 6.52
CHEMBL287887 1 6.52
CHEMBL88149 1 6.15
CHEMBL3392277 1 5.92
CHEMBL3392288 1 5.72
CHEMBL3392278 1 5.21
CHEMBL3392287 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL475534 NITRENDIPINE IC50 = 1.0 nM 9.00
CHEMBL3392282 IC50 = 4.0 nM 8.40
CHEMBL3392286 IC50 = 6.0 nM 8.22
CHEMBL2398396 IC50 = 7.0 nM 8.15
CHEMBL3392281 IC50 = 9.0 nM 8.05
CHEMBL3392283 IC50 = 16.0 nM 7.80
CHEMBL3392280 IC50 = 26.0 nM 7.58
CHEMBL3392284 IC50 = 30.0 nM 7.52
CHEMBL3392285 IC50 = 36.0 nM 7.44
CHEMBL39925 IC50 = 130.0 nM 6.89
CHEMBL3392289 IC50 = 170.0 nM 6.77
CHEMBL472962 IC50 = 180.0 nM 6.75
CHEMBL515270 IC50 = 190.0 nM 6.72
CHEMBL282279 IC50 = 280.0 nM 6.55
CHEMBL3392279 IC50 = 300.0 nM 6.52
CHEMBL287887 IC50 = 300.0 nM 6.52
CHEMBL88149 IC50 = 710.0 nM 6.15
CHEMBL3392277 IC50 = 1200.0 nM 5.92
CHEMBL3392288 IC50 = 1900.0 nM 5.72
CHEMBL3392278 IC50 = 6100.0 nM 5.21
CHEMBL3392287 IC50 > 100000.0 nM -