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Assay Detail

CHEMBL684573

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

Functional
Inhibition of tonic (slow) component of K+ depolarization response in guinea pig ileal longitudinal smooth muscle
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Tissue Muscle tissue
Confidence 1 — Organism
Curated By Expert

Target

Cavia porcellus (CHEMBL369)
Type ORGANISM
Organism Cavia porcellus

Publication

Crystal structures and pharmacologic activities of 1,4-dihydropyridine calcium channel antagonists of the isobutyl methyl 2,6-dimethyl-4-(substituted phenyl)-1,4-dihydropyridine-3,5-dicarboxylate (nisoldipine) series.
Fossheim R, Joslyn A, Solo AJ, Luchowski E, Rutledge A, Triggle DJ.
J Med Chem (1988) 31 : 300 -305
PubMed 3339603 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 8.59 9.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL441428 1 9.66
CHEMBL317044 1 9.57
CHEMBL102907 1 9.23
CHEMBL103806 1 8.68
CHEMBL105444 1 8.48
CHEMBL319033 1 8.17
CHEMBL102498 1 8.15
CHEMBL321999 1 7.82
CHEMBL318521 1 7.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL441428 IC50 = 0.22 nM 9.66
CHEMBL317044 IC50 = 0.27 nM 9.57
CHEMBL102907 IC50 = 0.59 nM 9.23
CHEMBL103806 IC50 = 2.1 nM 8.68
CHEMBL105444 IC50 = 3.3 nM 8.48
CHEMBL319033 IC50 = 6.8 nM 8.17
CHEMBL102498 IC50 = 7.1 nM 8.15
CHEMBL321999 IC50 = 15.0 nM 7.82
CHEMBL318521 IC50 = 27.0 nM 7.57