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Assay Detail

CHEMBL654566

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Binding
Inhibition of [3H]nitrendipine binding to L-type calcium channel from rat brain cortex homogenate
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Voltage-gated L-type calcium channel (CHEMBL2095177)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Stereoselectivity of a potent calcium antagonist, 1-benzyl-3-pyrrolidinyl methyl 2,6-dimethyl-4-(m-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate.
Tamazawa K, Arima H, Kojima T, Isomura Y, Okada M, Fujita S, Furuya T, Takenaka T, Inagaki O, Terai M.
J Med Chem (1986) 29 : 2504 -2511
PubMed 3023614 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 8.53 9.69

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2093893 1 9.69
CHEMBL1314450 1 9.30
CHEMBL1484 NICARDIPINE 4.0 1 9.08
CHEMBL558616 1 8.51
CHEMBL193 NIFEDIPINE 4.0 1 8.33
CHEMBL1598680 1 8.15
CHEMBL542169 1 7.84
CHEMBL553553 1 7.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2093893 Ki = 0.205 nM 9.69
CHEMBL1314450 Ki = 0.499 nM 9.30
CHEMBL1484 NICARDIPINE Ki = 0.84 nM 9.08
CHEMBL558616 Ki = 3.09 nM 8.51
CHEMBL193 NIFEDIPINE Ki = 4.65 nM 8.33
CHEMBL1598680 Ki = 7.11 nM 8.15
CHEMBL542169 Ki = 14.3 nM 7.84
CHEMBL553553 Ki = 49.6 nM 7.30