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Assay Detail

CHEMBL1909103

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

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

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Cerebral cortex
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 6.30 10.09
Ki 871 6.49 10.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1480 FELODIPINE 4.0 2 10.28
CHEMBL1428 NIMODIPINE 4.0 2 9.81
CHEMBL475534 NITRENDIPINE 3.0 2 9.61
CHEMBL460291 LACIDIPINE 3.0 2 9.59
CHEMBL1726 NISOLDIPINE 4.0 2 9.32
CHEMBL1491 AMLODIPINE 4.0 2 7.70
CHEMBL193 NIFEDIPINE 4.0 2 7.51
CHEMBL305660 EBASTINE 4.0 2 7.04
CHEMBL633 AMIODARONE 4.0 2 6.97
CHEMBL404849 SULOCTIDIL 4.0 2 6.78
CHEMBL81 RALOXIFENE 4.0 2 6.60
CHEMBL17157 TERFENADINE 4.0 2 6.30
CHEMBL772 RESERPINE 4.0 2 6.28
CHEMBL43064 CINNARIZINE 2.0 2 6.26
CHEMBL30008 FLUNARIZINE 2.0 2 6.19
CHEMBL490 PAROXETINE 4.0 2 6.02
CHEMBL1262 OXICONAZOLE 4.0 2 6.02
CHEMBL296419 ASTEMIZOLE 4.0 2 5.98
CHEMBL954 ENCLOMIPHENE 3.0 2 5.98
CHEMBL141343 — — 2 5.97
CHEMBL64894 GENTIAN VIOLET 4.0 2 5.86
CHEMBL1221 SULCONAZOLE 4.0 2 5.81
CHEMBL1221512 — — 2 5.54
CHEMBL808 ECONAZOLE 4.0 2 5.46
CHEMBL91 MICONAZOLE 4.0 2 5.39
CHEMBL104 CLOTRIMAZOLE 4.0 2 5.34
CHEMBL83 TAMOXIFEN 4.0 2 5.26
CHEMBL584 NELFINAVIR 4.0 2 5.20
CHEMBL672 FENOFIBRATE 4.0 2 4.95
CHEMBL1479 DANAZOL 4.0 2 4.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1480 FELODIPINE Ki = 0.053 nM 10.28
CHEMBL1480 FELODIPINE IC50 = 0.082 nM 10.09
CHEMBL1428 NIMODIPINE Ki = 0.156 nM 9.81
CHEMBL1428 NIMODIPINE IC50 = 0.242 nM 9.62
CHEMBL475534 NITRENDIPINE Ki = 0.246 nM 9.61
CHEMBL460291 LACIDIPINE Ki = 0.257 nM 9.59
CHEMBL475534 NITRENDIPINE IC50 = 0.383 nM 9.42
CHEMBL460291 LACIDIPINE IC50 = 0.4 nM 9.40
CHEMBL1726 NISOLDIPINE Ki = 0.476 nM 9.32
CHEMBL1726 NISOLDIPINE IC50 = 0.741 nM 9.13
CHEMBL1491 AMLODIPINE Ki = 20.0 nM 7.70
CHEMBL193 NIFEDIPINE Ki = 31.0 nM 7.51
CHEMBL1491 AMLODIPINE IC50 = 31.0 nM 7.51
CHEMBL193 NIFEDIPINE IC50 = 48.0 nM 7.32
CHEMBL305660 EBASTINE Ki = 92.3 nM 7.04
CHEMBL633 AMIODARONE Ki = 106.0 nM 6.97
CHEMBL305660 EBASTINE IC50 = 143.6 nM 6.84
CHEMBL633 AMIODARONE IC50 = 165.0 nM 6.78
CHEMBL404849 SULOCTIDIL Ki = 166.8 nM 6.78
CHEMBL81 RALOXIFENE Ki = 249.0 nM 6.60
CHEMBL404849 SULOCTIDIL IC50 = 259.5 nM 6.59
CHEMBL81 RALOXIFENE IC50 = 388.0 nM 6.41
CHEMBL17157 TERFENADINE Ki = 501.0 nM 6.30
CHEMBL772 RESERPINE Ki = 528.0 nM 6.28
CHEMBL43064 CINNARIZINE Ki = 544.0 nM 6.26
CHEMBL30008 FLUNARIZINE Ki = 650.0 nM 6.19
CHEMBL17157 TERFENADINE IC50 = 779.0 nM 6.11
CHEMBL772 RESERPINE IC50 = 821.0 nM 6.09
CHEMBL43064 CINNARIZINE IC50 = 846.0 nM 6.07
CHEMBL1262 OXICONAZOLE Ki = 945.7 nM 6.02
CHEMBL490 PAROXETINE Ki = 949.0 nM 6.02
CHEMBL30008 FLUNARIZINE IC50 = 1012.0 nM 6.00
CHEMBL296419 ASTEMIZOLE Ki = 1040.0 nM 5.98
CHEMBL954 ENCLOMIPHENE Ki = 1041.0 nM 5.98
CHEMBL141343 — Ki = 1066.0 nM 5.97
CHEMBL64894 GENTIAN VIOLET Ki = 1371.0 nM 5.86
CHEMBL490 PAROXETINE IC50 = 1476.0 nM 5.83
CHEMBL1262 OXICONAZOLE IC50 = 1471.1 nM 5.83
CHEMBL1221 SULCONAZOLE Ki = 1560.0 nM 5.81
CHEMBL296419 ASTEMIZOLE IC50 = 1617.0 nM 5.79
CHEMBL954 ENCLOMIPHENE IC50 = 1620.0 nM 5.79
CHEMBL141343 — IC50 = 1659.0 nM 5.78
CHEMBL64894 GENTIAN VIOLET IC50 = 2133.0 nM 5.67
CHEMBL1221 SULCONAZOLE IC50 = 2427.0 nM 5.62
CHEMBL1221512 — Ki = 2893.0 nM 5.54
CHEMBL808 ECONAZOLE Ki = 3506.0 nM 5.46
CHEMBL91 MICONAZOLE Ki = 4028.0 nM 5.39
CHEMBL1221512 — IC50 = 4501.0 nM 5.35
CHEMBL104 CLOTRIMAZOLE Ki = 4598.0 nM 5.34
CHEMBL808 ECONAZOLE IC50 = 5453.0 nM 5.26