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Assay Detail

CHEMBL771605

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

Functional
In vitro evaluation for the vasorelaxant effects in circumferential strips of potassium-depolarized rabbit aorta. (IC50 in rabbit aorta strips contracted with KCl)
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Oryctolagus cuniculus (CHEMBL374)
Type ORGANISM
Organism Oryctolagus cuniculus

Publication

Benzazepinone calcium channel blockers. 3. Synthesis and structure-activity studies of 3-alkylbenzazepinones.
Das J, Floyd DM, Kimball SD, Duff KJ, Vu TC, Lago MW, Moquin RV, Lee VG, Gougoutas JZ, Malley MF.
J Med Chem (1992) 35 : 773 -780
PubMed 1542103 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 6.69 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1204379 1 7.92
CHEMBL164515 1 7.77
CHEMBL1203799 1 7.16
CHEMBL1204374 1 7.11
CHEMBL350273 1 7.10
CHEMBL167935 1 7.10
CHEMBL1204375 1 7.05
CHEMBL348763 CLENTIAZEM 2.0 1 7.00
CHEMBL2093048 1 7.00
CHEMBL168068 1 6.82
CHEMBL433409 1 6.82
CHEMBL164658 1 6.80
CHEMBL1204378 1 6.72
CHEMBL23 DILTIAZEM 4.0 1 6.68
CHEMBL1203798 1 6.62
CHEMBL348847 1 6.55
CHEMBL1204377 1 6.47
CHEMBL1204376 1 6.38
CHEMBL163839 1 6.10
CHEMBL1204373 1 6.02
CHEMBL1204308 1 5.96
CHEMBL1203797 1 5.92
CHEMBL1203795 1 5.91
CHEMBL1203796 1 5.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1204379 IC50 = 12.0 nM 7.92
CHEMBL164515 IC50 = 17.0 nM 7.77
CHEMBL1203799 IC50 = 70.0 nM 7.16
CHEMBL1204374 IC50 = 77.0 nM 7.11
CHEMBL350273 IC50 = 80.0 nM 7.10
CHEMBL167935 IC50 = 80.0 nM 7.10
CHEMBL1204375 IC50 = 90.0 nM 7.05
CHEMBL348763 CLENTIAZEM IC50 = 100.0 nM 7.00
CHEMBL2093048 IC50 = 100.0 nM 7.00
CHEMBL168068 IC50 = 150.0 nM 6.82
CHEMBL433409 IC50 = 150.0 nM 6.82
CHEMBL164658 IC50 = 160.0 nM 6.80
CHEMBL1204378 IC50 = 190.0 nM 6.72
CHEMBL23 DILTIAZEM IC50 = 210.0 nM 6.68
CHEMBL1203798 IC50 = 240.0 nM 6.62
CHEMBL348847 IC50 = 280.0 nM 6.55
CHEMBL1204377 IC50 = 340.0 nM 6.47
CHEMBL1204376 IC50 = 420.0 nM 6.38
CHEMBL163839 IC50 = 790.0 nM 6.10
CHEMBL1204373 IC50 = 950.0 nM 6.02
CHEMBL1204308 IC50 = 1100.0 nM 5.96
CHEMBL1203797 IC50 = 1200.0 nM 5.92
CHEMBL1203795 IC50 = 1230.0 nM 5.91
CHEMBL1203796 IC50 = 3290.0 nM 5.48