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Assay Detail

CHEMBL844574

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

Functional
Calcium antagonistic activity assessed against calcium-induced constriction of potassium-depolarized rat aorta.
40
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Aorta
Confidence 1 — Organism
Curated By Expert

Target

Rattus norvegicus (CHEMBL376)
Type ORGANISM
Organism Rattus norvegicus

Publication

A new class of calcium antagonists. Synthesis and biological activity of 11-[(omega-aminoalkanoyl)amino]-6,6a,7,8,9,10,10a,11-octahydrodibenzo [b,e]thiepin derivatives.
Kurokawa M, Sato F, Hatano N, Honda Y, Uno H.
J Med Chem (1991) 34 : 593 -599
PubMed 1995882 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 40 7.34 8.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL157248 1 8.16
CHEMBL157859 1 8.15
CHEMBL346483 1 8.05
CHEMBL350910 1 7.82
CHEMBL156962 1 7.82
CHEMBL155550 1 7.80
CHEMBL422350 1 7.77
CHEMBL154726 1 7.73
CHEMBL154721 1 7.72
CHEMBL1788142 1 7.68
CHEMBL347430 1 7.60
CHEMBL435233 1 7.57
CHEMBL434848 1 7.57
CHEMBL346147 1 7.55
CHEMBL154172 1 7.52
CHEMBL158191 1 7.52
CHEMBL23 DILTIAZEM 4.0 1 7.42
CHEMBL155266 1 7.39
CHEMBL154266 1 7.38
CHEMBL421803 1 7.34
CHEMBL345164 1 7.33
CHEMBL346313 1 7.26
CHEMBL422341 1 7.25
CHEMBL345224 1 7.24
CHEMBL345239 1 7.24
CHEMBL156410 1 7.16
CHEMBL345856 1 7.15
CHEMBL154365 1 7.15
CHEMBL436426 1 7.14
CHEMBL154474 1 7.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL157248 Kd = 6.918 nM 8.16
CHEMBL157859 Kd = 7.079 nM 8.15
CHEMBL346483 Kd = 8.913 nM 8.05
CHEMBL350910 Kd = 15.14 nM 7.82
CHEMBL156962 Kd = 15.14 nM 7.82
CHEMBL155550 Kd = 15.85 nM 7.80
CHEMBL422350 Kd = 16.98 nM 7.77
CHEMBL154726 Kd = 18.62 nM 7.73
CHEMBL154721 Kd = 19.05 nM 7.72
CHEMBL1788142 Kd = 20.89 nM 7.68
CHEMBL347430 Kd = 25.12 nM 7.60
CHEMBL435233 Kd = 26.92 nM 7.57
CHEMBL434848 Kd = 26.92 nM 7.57
CHEMBL346147 Kd = 28.18 nM 7.55
CHEMBL158191 Kd = 30.2 nM 7.52
CHEMBL154172 Kd = 30.2 nM 7.52
CHEMBL23 DILTIAZEM Kd = 38.02 nM 7.42
CHEMBL155266 Kd = 40.74 nM 7.39
CHEMBL154266 Kd = 41.69 nM 7.38
CHEMBL421803 Kd = 45.71 nM 7.34
CHEMBL345164 Kd = 46.77 nM 7.33
CHEMBL346313 Kd = 54.95 nM 7.26
CHEMBL422341 Kd = 56.23 nM 7.25
CHEMBL345239 Kd = 57.54 nM 7.24
CHEMBL345224 Kd = 57.54 nM 7.24
CHEMBL156410 Kd = 69.18 nM 7.16
CHEMBL345856 Kd = 70.79 nM 7.15
CHEMBL154365 Kd = 70.79 nM 7.15
CHEMBL436426 Kd = 72.44 nM 7.14
CHEMBL154474 Kd = 75.86 nM 7.12
CHEMBL345743 Kd = 77.62 nM 7.11
CHEMBL157514 Kd = 81.28 nM 7.09
CHEMBL345403 Kd = 97.72 nM 7.01
CHEMBL154559 Kd = 104.71 nM 6.98
CHEMBL154707 Kd = 138.04 nM 6.86
CHEMBL436040 Kd = 141.25 nM 6.85
CHEMBL422863 Kd = 158.49 nM 6.80
CHEMBL155713 Kd = 323.59 nM 6.49
CHEMBL155713 Kd = 331.13 nM 6.48
CHEMBL346991 Kd = 416.87 nM 6.38