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Assay Detail

CHEMBL703977

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

Binding
Inhibition of [3H]nitrendipine binding to L-type [Ca2+] channel in rat cortex homogenate, activity expressed as pIC50
39
Total Activities
39
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Cortex
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Voltage-dependent L-type calcium channel subunit alpha-1D (CHEMBL4132)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Diltiazem-like calcium entry blockers: a hypothesis of the receptor-binding site based on a comparative molecular field analysis model.
Corelli F, Manetti F, Tafi A, Campiani G, Nacci V, Botta M.
J Med Chem (1997) 40 : 125 -131
PubMed 9016337 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 39 6.61 9.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL277363 1 9.37
CHEMBL24662 1 9.11
CHEMBL278804 1 8.48
CHEMBL25512 1 8.36
CHEMBL24998 1 7.92
CHEMBL18988 1 7.82
CHEMBL25278 1 7.66
CHEMBL284195 1 7.54
CHEMBL282348 1 7.52
CHEMBL23 DILTIAZEM 4.0 1 7.34
CHEMBL24675 1 7.28
CHEMBL282651 1 7.19
CHEMBL24086 1 7.09
CHEMBL26172 1 6.97
CHEMBL283615 1 6.87
CHEMBL275195 1 6.82
CHEMBL282989 1 6.70
CHEMBL24085 1 6.66
CHEMBL25124 1 6.52
CHEMBL278171 1 6.50
CHEMBL277293 1 6.50
CHEMBL287410 1 6.40
CHEMBL26495 1 6.33
CHEMBL287054 1 6.11
CHEMBL24529 1 5.91
CHEMBL281762 1 5.91
CHEMBL280391 1 5.80
CHEMBL282854 1 5.80
CHEMBL24243 1 5.69
CHEMBL279886 1 5.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL277363 IC50 = 0.4266 nM 9.37
CHEMBL24662 IC50 = 0.7762 nM 9.11
CHEMBL278804 IC50 = 3.311 nM 8.48
CHEMBL25512 IC50 = 4.365 nM 8.36
CHEMBL24998 IC50 = 12.02 nM 7.92
CHEMBL18988 IC50 = 15.14 nM 7.82
CHEMBL25278 IC50 = 21.88 nM 7.66
CHEMBL284195 IC50 = 28.84 nM 7.54
CHEMBL282348 IC50 = 30.2 nM 7.52
CHEMBL23 DILTIAZEM IC50 = 45.71 nM 7.34
CHEMBL24675 IC50 = 52.48 nM 7.28
CHEMBL282651 IC50 = 64.57 nM 7.19
CHEMBL24086 IC50 = 81.28 nM 7.09
CHEMBL26172 IC50 = 107.15 nM 6.97
CHEMBL283615 IC50 = 134.9 nM 6.87
CHEMBL275195 IC50 = 151.36 nM 6.82
CHEMBL282989 IC50 = 199.53 nM 6.70
CHEMBL24085 IC50 = 218.78 nM 6.66
CHEMBL25124 IC50 = 302.0 nM 6.52
CHEMBL278171 IC50 = 316.23 nM 6.50
CHEMBL277293 IC50 = 316.23 nM 6.50
CHEMBL287410 IC50 = 398.11 nM 6.40
CHEMBL26495 IC50 = 467.74 nM 6.33
CHEMBL287054 IC50 = 776.25 nM 6.11
CHEMBL24529 IC50 = 1230.27 nM 5.91
CHEMBL281762 IC50 = 1230.27 nM 5.91
CHEMBL280391 IC50 = 1584.89 nM 5.80
CHEMBL282854 IC50 = 1584.89 nM 5.80
CHEMBL24243 IC50 = 2041.74 nM 5.69
CHEMBL279886 IC50 = 2187.76 nM 5.66
CHEMBL26442 IC50 = 4365.16 nM 5.36
CHEMBL26605 IC50 = 4677.35 nM 5.33
CHEMBL429774 IC50 = 5011.87 nM 5.30
CHEMBL442147 IC50 = 5011.87 nM 5.30
CHEMBL26239 IC50 = 5011.87 nM 5.30
CHEMBL281664 IC50 = 5011.87 nM 5.30
CHEMBL24620 IC50 = 5011.87 nM 5.30
CHEMBL281311 IC50 = 5011.87 nM 5.30
CHEMBL283244 IC50 = 5011.87 nM 5.30