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Assay Detail

CHEMBL857764

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

Functional
Inhibitory concentration of [3H]- nitrendipine binding against guinea pig cerebral cortex membrane
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Tissue Cerebral cortex
Subcellular Membrane
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Novel heterocyclic analogues of the new potent class of calcium entry blockers: 1-[[4-(aminoalkoxy)phenyl]sulfonyl]indolizines.
Gubin J, de Vogelaer H, Inion H, Houben C, Lucchetti J, Mahaux J, Rosseels G, Peiren M, Clinet M, Polster P.
J Med Chem (1993) 36 : 1425 -1433
PubMed 8496910 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 8.28 10.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL33620 1 10.14
CHEMBL34509 1 10.03
CHEMBL32989 1 9.66
CHEMBL34685 1 9.55
CHEMBL33344 1 9.23
CHEMBL285855 FANTOFARONE 2.0 1 9.21
CHEMBL34058 1 9.19
CHEMBL31082 1 9.00
CHEMBL30440 1 9.00
CHEMBL287679 1 8.96
CHEMBL33001 1 8.80
CHEMBL33326 1 8.72
CHEMBL34450 1 8.66
CHEMBL193 NIFEDIPINE 4.0 1 8.60
CHEMBL33293 1 8.59
CHEMBL417136 1 8.28
CHEMBL34100 1 8.14
CHEMBL33559 1 8.10
CHEMBL33072 1 7.96
CHEMBL30535 1 7.96
CHEMBL33560 1 7.92
CHEMBL30321 1 7.88
CHEMBL33738 1 7.87
CHEMBL6966 VERAPAMIL 4.0 1 7.42
CHEMBL33735 1 7.03
CHEMBL281749 1 6.96
CHEMBL418045 1 6.94
CHEMBL33497 1 6.82
CHEMBL33531 1 6.74
CHEMBL33740 1 6.73

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL33620 IC50 = 0.072 nM 10.14
CHEMBL34509 IC50 = 0.093 nM 10.03
CHEMBL32989 IC50 = 0.22 nM 9.66
CHEMBL34685 IC50 = 0.28 nM 9.55
CHEMBL33344 IC50 = 0.59 nM 9.23
CHEMBL285855 FANTOFARONE IC50 = 0.61 nM 9.21
CHEMBL34058 IC50 = 0.65 nM 9.19
CHEMBL31082 IC50 = 1.0 nM 9.00
CHEMBL30440 IC50 = 0.99 nM 9.00
CHEMBL287679 IC50 = 1.1 nM 8.96
CHEMBL33001 IC50 = 1.6 nM 8.80
CHEMBL33326 IC50 = 1.9 nM 8.72
CHEMBL34450 IC50 = 2.2 nM 8.66
CHEMBL193 NIFEDIPINE IC50 = 2.5 nM 8.60
CHEMBL33293 IC50 = 2.6 nM 8.59
CHEMBL417136 IC50 = 5.2 nM 8.28
CHEMBL34100 IC50 = 7.2 nM 8.14
CHEMBL33559 IC50 = 7.9 nM 8.10
CHEMBL33072 IC50 = 11.0 nM 7.96
CHEMBL30535 IC50 = 10.9 nM 7.96
CHEMBL33560 IC50 = 12.0 nM 7.92
CHEMBL30321 IC50 = 13.1 nM 7.88
CHEMBL33738 IC50 = 13.6 nM 7.87
CHEMBL6966 VERAPAMIL IC50 = 38.0 nM 7.42
CHEMBL33735 IC50 = 94.0 nM 7.03
CHEMBL281749 IC50 = 110.0 nM 6.96
CHEMBL418045 IC50 = 116.0 nM 6.94
CHEMBL33497 IC50 = 151.0 nM 6.82
CHEMBL33531 IC50 = 181.0 nM 6.74
CHEMBL33740 IC50 = 186.0 nM 6.73
CHEMBL30954 IC50 = 244.0 nM 6.61