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Assay Detail

CHEMBL1909086

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

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

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Liver
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Alpha-1B adrenergic receptor (CHEMBL315)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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 6.79 9.75
Ki 871 7.05 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2 PRAZOSIN 4.0 2 10.00
CHEMBL707 DOXAZOSIN 4.0 2 9.38
CHEMBL85 RISPERIDONE 4.0 2 8.97
CHEMBL1255837 DIHYDROERGOCRISTINE MESYLATE 2 8.90
CHEMBL1909072 PIPAMAZINE 4.0 2 8.85
CHEMBL493 BROMOCRIPTINE 4.0 2 8.71
CHEMBL723 CARVEDILOL 4.0 2 8.71
CHEMBL479 THIORIDAZINE 4.0 2 8.59
CHEMBL1385840 ERGOCORNINE 2 8.54
CHEMBL611 TERAZOSIN 4.0 2 8.48
CHEMBL42 CLOZAPINE 4.0 2 8.45
CHEMBL1732 DIHYDROERGOTAMINE 4.0 2 8.35
CHEMBL442 ERGOTAMINE 4.0 2 8.34
CHEMBL564 PROMAZINE 4.0 2 8.34
CHEMBL54 HALOPERIDOL 4.0 2 8.31
CHEMBL71 CHLORPROMAZINE 4.0 2 8.30
CHEMBL1403281 ERGOCRYPTINE 2 8.10
CHEMBL1729 CISAPRIDE 4.0 2 8.06
CHEMBL1108 DROPERIDOL 4.0 2 8.01
CHEMBL716 QUETIAPINE 4.0 2 7.87
CHEMBL726 FLUPHENAZINE 4.0 2 7.72
CHEMBL643 PROMETHAZINE 4.0 2 7.68
CHEMBL715 OLANZAPINE 4.0 2 7.68
CHEMBL1201216 DAPIPRAZOLE 4.0 2 7.52
CHEMBL1628227 DOXEPIN 4.0 2 7.48
CHEMBL395110 MEPAZINE 4.0 2 7.47
CHEMBL1201203 BENZTROPINE 4.0 2 7.39
CHEMBL1626 CLEMASTINE 4.0 2 7.39
CHEMBL629 AMITRIPTYLINE 4.0 2 7.38
CHEMBL516 CYPROHEPTADINE 4.0 2 7.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2 PRAZOSIN Ki = 0.099 nM 10.00
CHEMBL2 PRAZOSIN IC50 = 0.178 nM 9.75
CHEMBL707 DOXAZOSIN Ki = 0.416 nM 9.38
CHEMBL707 DOXAZOSIN IC50 = 0.751 nM 9.12
CHEMBL85 RISPERIDONE Ki = 1.079 nM 8.97
CHEMBL1255837 DIHYDROERGOCRISTINE MESYLATE Ki = 1.272 nM 8.90
CHEMBL1909072 PIPAMAZINE Ki = 1.417 nM 8.85
CHEMBL723 CARVEDILOL Ki = 1.966 nM 8.71
CHEMBL85 RISPERIDONE IC50 = 1.949 nM 8.71
CHEMBL493 BROMOCRIPTINE Ki = 1.964 nM 8.71
CHEMBL1255837 DIHYDROERGOCRISTINE MESYLATE IC50 = 2.298 nM 8.64
CHEMBL1909072 PIPAMAZINE IC50 = 2.56 nM 8.59
CHEMBL479 THIORIDAZINE Ki = 2.597 nM 8.59
CHEMBL1385840 ERGOCORNINE Ki = 2.873 nM 8.54
CHEMBL611 TERAZOSIN Ki = 3.335 nM 8.48
CHEMBL42 CLOZAPINE Ki = 3.591 nM 8.45
CHEMBL723 CARVEDILOL IC50 = 3.551 nM 8.45
CHEMBL493 BROMOCRIPTINE IC50 = 3.547 nM 8.45
CHEMBL1732 DIHYDROERGOTAMINE Ki = 4.477 nM 8.35
CHEMBL564 PROMAZINE Ki = 4.532 nM 8.34
CHEMBL442 ERGOTAMINE Ki = 4.547 nM 8.34
CHEMBL479 THIORIDAZINE IC50 = 4.692 nM 8.33
CHEMBL54 HALOPERIDOL Ki = 4.946 nM 8.31
CHEMBL71 CHLORPROMAZINE Ki = 4.963 nM 8.30
CHEMBL1385840 ERGOCORNINE IC50 = 5.19 nM 8.29
CHEMBL611 TERAZOSIN IC50 = 6.025 nM 8.22
CHEMBL42 CLOZAPINE IC50 = 6.487 nM 8.19
CHEMBL1403281 ERGOCRYPTINE Ki = 7.938 nM 8.10
CHEMBL1732 DIHYDROERGOTAMINE IC50 = 8.088 nM 8.09
CHEMBL564 PROMAZINE IC50 = 8.187 nM 8.09
CHEMBL442 ERGOTAMINE IC50 = 8.214 nM 8.09
CHEMBL1729 CISAPRIDE Ki = 8.654 nM 8.06
CHEMBL71 CHLORPROMAZINE IC50 = 8.966 nM 8.05
CHEMBL54 HALOPERIDOL IC50 = 8.935 nM 8.05
CHEMBL1108 DROPERIDOL Ki = 9.78 nM 8.01
CHEMBL716 QUETIAPINE Ki = 13.6 nM 7.87
CHEMBL1403281 ERGOCRYPTINE IC50 = 14.0 nM 7.85
CHEMBL1729 CISAPRIDE IC50 = 16.0 nM 7.80
CHEMBL1108 DROPERIDOL IC50 = 18.0 nM 7.75
CHEMBL726 FLUPHENAZINE Ki = 19.0 nM 7.72
CHEMBL715 OLANZAPINE Ki = 21.0 nM 7.68
CHEMBL643 PROMETHAZINE Ki = 21.0 nM 7.68
CHEMBL716 QUETIAPINE IC50 = 24.5 nM 7.61
CHEMBL1201216 DAPIPRAZOLE Ki = 30.0 nM 7.52
CHEMBL1628227 DOXEPIN Ki = 33.0 nM 7.48
CHEMBL726 FLUPHENAZINE IC50 = 34.0 nM 7.47
CHEMBL395110 MEPAZINE Ki = 34.0 nM 7.47
CHEMBL715 OLANZAPINE IC50 = 37.0 nM 7.43
CHEMBL643 PROMETHAZINE IC50 = 39.0 nM 7.41
CHEMBL1201203 BENZTROPINE Ki = 41.0 nM 7.39