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Assay Detail

CHEMBL1909121

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

Binding
DRUGMATRIX: Calcium Channel Type L, Phenylalkylamine radioligand binding (ligand: [3H] (-)-Desmethoxyverapamil (D-888))
ChEMBL ↗
1742
Total Activities
871
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Subcellular Membrane
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545) ↗
Type UNCHECKED

Publication

DrugMatrix in vitro pharmacology data
Scott S. Auerbach, DrugMatrix¨ and ToxFX¨ Coordinator National Toxicology Program

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 871 5.84 7.33
Ki 871 5.85 7.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6966 VERAPAMIL 4.0 2 7.35
CHEMBL1123 DICYCLOMINE 4.0 2 6.97
CHEMBL305660 EBASTINE 4.0 2 6.94
CHEMBL81 RALOXIFENE 4.0 2 6.84
CHEMBL30008 FLUNARIZINE 2.0 2 6.76
CHEMBL19215 METERGOLINE 2.0 2 6.57
CHEMBL296419 ASTEMIZOLE 4.0 2 6.53
CHEMBL723 CARVEDILOL 4.0 2 6.42
CHEMBL516 CYPROHEPTADINE 4.0 2 6.37
CHEMBL479 THIORIDAZINE 4.0 2 6.37
CHEMBL221753 BENZETHONIUM CHLORIDE 2.0 2 6.36
CHEMBL21731 MAPROTILINE 4.0 2 6.36
CHEMBL1626 CLEMASTINE 4.0 2 6.31
CHEMBL415 CLOMIPRAMINE 4.0 2 6.31
CHEMBL404849 SULOCTIDIL 4.0 2 6.29
CHEMBL1729 CISAPRIDE 4.0 2 6.29
CHEMBL633 AMIODARONE 4.0 2 6.28
CHEMBL1628227 DOXEPIN 4.0 2 6.28
CHEMBL54 HALOPERIDOL 4.0 2 6.27
CHEMBL841 LOPERAMIDE 4.0 2 6.24
CHEMBL42 CLOZAPINE 4.0 2 6.22
CHEMBL43064 CINNARIZINE 2.0 2 6.22
CHEMBL17157 TERFENADINE 4.0 2 6.22
CHEMBL23 DILTIAZEM 4.0 2 6.21
CHEMBL490 PAROXETINE 4.0 2 6.14
CHEMBL597 PHENTOLAMINE 4.0 2 6.14
CHEMBL7568 QUINACRINE 4.0 2 6.14
CHEMBL954 ENCLOMIPHENE 3.0 2 6.13
CHEMBL629 AMITRIPTYLINE 4.0 2 6.09
CHEMBL643 PROMETHAZINE 4.0 2 6.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6966 VERAPAMIL Ki = 45.0 nM 7.35
CHEMBL6966 VERAPAMIL IC50 = 47.0 nM 7.33
CHEMBL1123 DICYCLOMINE Ki = 107.0 nM 6.97
CHEMBL1123 DICYCLOMINE IC50 = 110.0 nM 6.96
CHEMBL305660 EBASTINE Ki = 115.2 nM 6.94
CHEMBL305660 EBASTINE IC50 = 118.5 nM 6.93
CHEMBL81 RALOXIFENE Ki = 144.0 nM 6.84
CHEMBL81 RALOXIFENE IC50 = 148.0 nM 6.83
CHEMBL30008 FLUNARIZINE Ki = 172.0 nM 6.76
CHEMBL30008 FLUNARIZINE IC50 = 177.0 nM 6.75
CHEMBL19215 METERGOLINE Ki = 270.0 nM 6.57
CHEMBL19215 METERGOLINE IC50 = 278.0 nM 6.56
CHEMBL296419 ASTEMIZOLE Ki = 296.0 nM 6.53
CHEMBL296419 ASTEMIZOLE IC50 = 305.0 nM 6.52
CHEMBL723 CARVEDILOL Ki = 378.0 nM 6.42
CHEMBL723 CARVEDILOL IC50 = 389.0 nM 6.41
CHEMBL516 CYPROHEPTADINE Ki = 426.0 nM 6.37
CHEMBL479 THIORIDAZINE Ki = 431.0 nM 6.37
CHEMBL516 CYPROHEPTADINE IC50 = 438.0 nM 6.36
CHEMBL221753 BENZETHONIUM CHLORIDE Ki = 439.0 nM 6.36
CHEMBL21731 MAPROTILINE Ki = 434.0 nM 6.36
CHEMBL479 THIORIDAZINE IC50 = 443.0 nM 6.35
CHEMBL21731 MAPROTILINE IC50 = 446.0 nM 6.35
CHEMBL221753 BENZETHONIUM CHLORIDE IC50 = 452.0 nM 6.34
CHEMBL415 CLOMIPRAMINE Ki = 492.0 nM 6.31
CHEMBL1626 CLEMASTINE Ki = 493.0 nM 6.31
CHEMBL415 CLOMIPRAMINE IC50 = 506.0 nM 6.30
CHEMBL1626 CLEMASTINE IC50 = 508.0 nM 6.29
CHEMBL1729 CISAPRIDE Ki = 515.0 nM 6.29
CHEMBL404849 SULOCTIDIL Ki = 510.5 nM 6.29
CHEMBL633 AMIODARONE Ki = 524.0 nM 6.28
CHEMBL404849 SULOCTIDIL IC50 = 525.1 nM 6.28
CHEMBL1729 CISAPRIDE IC50 = 530.0 nM 6.28
CHEMBL1628227 DOXEPIN Ki = 520.0 nM 6.28
CHEMBL633 AMIODARONE IC50 = 539.0 nM 6.27
CHEMBL54 HALOPERIDOL Ki = 536.0 nM 6.27
CHEMBL1628227 DOXEPIN IC50 = 535.0 nM 6.27
CHEMBL54 HALOPERIDOL IC50 = 552.0 nM 6.26
CHEMBL841 LOPERAMIDE Ki = 573.0 nM 6.24
CHEMBL841 LOPERAMIDE IC50 = 589.0 nM 6.23
CHEMBL43064 CINNARIZINE Ki = 607.0 nM 6.22
CHEMBL17157 TERFENADINE Ki = 607.0 nM 6.22
CHEMBL42 CLOZAPINE Ki = 595.0 nM 6.22
CHEMBL17157 TERFENADINE IC50 = 624.0 nM 6.21
CHEMBL42 CLOZAPINE IC50 = 612.0 nM 6.21
CHEMBL43064 CINNARIZINE IC50 = 624.0 nM 6.21
CHEMBL23 DILTIAZEM Ki = 612.0 nM 6.21
CHEMBL23 DILTIAZEM IC50 = 630.0 nM 6.20
CHEMBL490 PAROXETINE Ki = 726.0 nM 6.14
CHEMBL7568 QUINACRINE Ki = 719.0 nM 6.14