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Assay Detail

CHEMBL1909087

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

Binding
DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)
ChEMBL ↗
1742
Total Activities
871
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HEK293
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Alpha-1D adrenergic receptor (CHEMBL223) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

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 6.62 9.18
Ki 871 6.93 9.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2 PRAZOSIN 4.0 2 9.49
CHEMBL723 CARVEDILOL 4.0 2 9.05
CHEMBL1909072 PIPAMAZINE 4.0 2 9.02
CHEMBL707 DOXAZOSIN 4.0 2 8.78
CHEMBL71 CHLORPROMAZINE 4.0 2 8.71
CHEMBL479 THIORIDAZINE 4.0 2 8.54
CHEMBL1255837 DIHYDROERGOCRISTINE MESYLATE — 2 8.44
CHEMBL1201216 DAPIPRAZOLE 4.0 2 8.39
CHEMBL85 RISPERIDONE 4.0 2 8.31
CHEMBL564 PROMAZINE 4.0 2 8.21
CHEMBL611 TERAZOSIN 4.0 2 8.08
CHEMBL1385840 ERGOCORNINE — 2 8.06
CHEMBL597 PHENTOLAMINE 4.0 2 7.96
CHEMBL1732 DIHYDROERGOTAMINE 4.0 2 7.85
CHEMBL1626 CLEMASTINE 4.0 2 7.82
CHEMBL493 BROMOCRIPTINE 4.0 2 7.82
CHEMBL726 FLUPHENAZINE 4.0 2 7.80
CHEMBL728 PROCHLORPERAZINE 4.0 2 7.80
CHEMBL42 CLOZAPINE 4.0 2 7.77
CHEMBL157138 LISURIDE 3.0 2 7.70
CHEMBL1403281 ERGOCRYPTINE — 2 7.62
CHEMBL442 ERGOTAMINE 4.0 2 7.62
CHEMBL1201203 BENZTROPINE 4.0 2 7.58
CHEMBL1108 DROPERIDOL 4.0 2 7.39
CHEMBL54 HALOPERIDOL 4.0 2 7.39
CHEMBL6437 MIANSERIN 4.0 2 7.39
CHEMBL715 OLANZAPINE 4.0 2 7.35
CHEMBL716 QUETIAPINE 4.0 2 7.32
CHEMBL629 AMITRIPTYLINE 4.0 2 7.28
CHEMBL516 CYPROHEPTADINE 4.0 2 7.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2 PRAZOSIN Ki = 0.323 nM 9.49
CHEMBL2 PRAZOSIN IC50 = 0.656 nM 9.18
CHEMBL723 CARVEDILOL Ki = 0.883 nM 9.05
CHEMBL1909072 PIPAMAZINE Ki = 0.955 nM 9.02
CHEMBL707 DOXAZOSIN Ki = 1.663 nM 8.78
CHEMBL723 CARVEDILOL IC50 = 1.796 nM 8.75
CHEMBL71 CHLORPROMAZINE Ki = 1.962 nM 8.71
CHEMBL1909072 PIPAMAZINE IC50 = 1.944 nM 8.71
CHEMBL479 THIORIDAZINE Ki = 2.895 nM 8.54
CHEMBL707 DOXAZOSIN IC50 = 3.383 nM 8.47
CHEMBL1255837 DIHYDROERGOCRISTINE MESYLATE Ki = 3.622 nM 8.44
CHEMBL71 CHLORPROMAZINE IC50 = 3.991 nM 8.40
CHEMBL1201216 DAPIPRAZOLE Ki = 4.086 nM 8.39
CHEMBL85 RISPERIDONE Ki = 4.913 nM 8.31
CHEMBL479 THIORIDAZINE IC50 = 5.891 nM 8.23
CHEMBL564 PROMAZINE Ki = 6.18 nM 8.21
CHEMBL1255837 DIHYDROERGOCRISTINE MESYLATE IC50 = 7.369 nM 8.13
CHEMBL1201216 DAPIPRAZOLE IC50 = 8.312 nM 8.08
CHEMBL611 TERAZOSIN Ki = 8.363 nM 8.08
CHEMBL1385840 ERGOCORNINE Ki = 8.747 nM 8.06
CHEMBL85 RISPERIDONE IC50 = 9.995 nM 8.00
CHEMBL597 PHENTOLAMINE Ki = 11.0 nM 7.96
CHEMBL564 PROMAZINE IC50 = 13.0 nM 7.89
CHEMBL1732 DIHYDROERGOTAMINE Ki = 14.0 nM 7.85
CHEMBL493 BROMOCRIPTINE Ki = 15.0 nM 7.82
CHEMBL1626 CLEMASTINE Ki = 15.0 nM 7.82
CHEMBL728 PROCHLORPERAZINE Ki = 16.0 nM 7.80
CHEMBL726 FLUPHENAZINE Ki = 16.0 nM 7.80
CHEMBL611 TERAZOSIN IC50 = 17.0 nM 7.77
CHEMBL42 CLOZAPINE Ki = 17.0 nM 7.77
CHEMBL1385840 ERGOCORNINE IC50 = 18.0 nM 7.75
CHEMBL157138 LISURIDE Ki = 20.0 nM 7.70
CHEMBL597 PHENTOLAMINE IC50 = 22.0 nM 7.66
CHEMBL1403281 ERGOCRYPTINE Ki = 24.0 nM 7.62
CHEMBL442 ERGOTAMINE Ki = 24.0 nM 7.62
CHEMBL1201203 BENZTROPINE Ki = 26.0 nM 7.58
CHEMBL1732 DIHYDROERGOTAMINE IC50 = 29.0 nM 7.54
CHEMBL493 BROMOCRIPTINE IC50 = 30.0 nM 7.52
CHEMBL1626 CLEMASTINE IC50 = 32.0 nM 7.50
CHEMBL726 FLUPHENAZINE IC50 = 33.0 nM 7.48
CHEMBL728 PROCHLORPERAZINE IC50 = 34.0 nM 7.47
CHEMBL42 CLOZAPINE IC50 = 35.0 nM 7.46
CHEMBL6437 MIANSERIN Ki = 41.0 nM 7.39
CHEMBL54 HALOPERIDOL Ki = 41.0 nM 7.39
CHEMBL157138 LISURIDE IC50 = 41.0 nM 7.39
CHEMBL1108 DROPERIDOL Ki = 41.0 nM 7.39
CHEMBL715 OLANZAPINE Ki = 45.0 nM 7.35
CHEMBL1403281 ERGOCRYPTINE IC50 = 48.0 nM 7.32
CHEMBL716 QUETIAPINE Ki = 47.5 nM 7.32
CHEMBL442 ERGOTAMINE IC50 = 49.0 nM 7.31