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Assay Detail

CHEMBL1909089

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

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

Assay Information

Assay Type Binding
Cell Type CHO-K1
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Alpha-2B adrenergic receptor (CHEMBL1942) ↗
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 6.32 9.29
Ki 871 6.66 9.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL157138 LISURIDE 3.0 2 9.62
CHEMBL1909072 PIPAMAZINE 4.0 2 9.11
CHEMBL1385840 ERGOCORNINE — 2 8.86
CHEMBL442 ERGOTAMINE 4.0 2 8.76
CHEMBL1732 DIHYDROERGOTAMINE 4.0 2 8.75
CHEMBL1255837 DIHYDROERGOCRISTINE MESYLATE — 2 8.44
CHEMBL629 AMITRIPTYLINE 4.0 2 8.43
CHEMBL728 PROCHLORPERAZINE 4.0 2 8.32
CHEMBL19215 METERGOLINE 2.0 2 8.12
CHEMBL15245 YOHIMBINE 3.0 2 8.10
CHEMBL597 PHENTOLAMINE 4.0 2 8.09
CHEMBL564 PROMAZINE 4.0 2 8.07
CHEMBL42 CLOZAPINE 4.0 2 7.96
CHEMBL1909065 MADURAMICIN ACID 2.0 2 7.92
CHEMBL85 RISPERIDONE 4.0 2 7.92
CHEMBL71 CHLORPROMAZINE 4.0 2 7.92
CHEMBL1403281 ERGOCRYPTINE — 2 7.92
CHEMBL726 FLUPHENAZINE 4.0 2 7.89
CHEMBL493 BROMOCRIPTINE 4.0 2 7.80
CHEMBL516 CYPROHEPTADINE 4.0 2 7.77
CHEMBL643 PROMETHAZINE 4.0 2 7.62
CHEMBL6437 MIANSERIN 4.0 2 7.62
CHEMBL531 PERGOLIDE 4.0 2 7.54
CHEMBL1201203 BENZTROPINE 4.0 2 7.52
CHEMBL1628227 DOXEPIN 4.0 2 7.50
CHEMBL134 CLONIDINE 4.0 2 7.42
CHEMBL723 CARVEDILOL 4.0 2 7.37
CHEMBL445 NORTRIPTYLINE 4.0 2 7.37
CHEMBL415 CLOMIPRAMINE 4.0 2 7.34
CHEMBL716 QUETIAPINE 4.0 2 7.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL157138 LISURIDE Ki = 0.237 nM 9.62
CHEMBL157138 LISURIDE IC50 = 0.518 nM 9.29
CHEMBL1909072 PIPAMAZINE Ki = 0.786 nM 9.11
CHEMBL1385840 ERGOCORNINE Ki = 1.396 nM 8.86
CHEMBL442 ERGOTAMINE Ki = 1.755 nM 8.76
CHEMBL1909072 PIPAMAZINE IC50 = 1.722 nM 8.76
CHEMBL1732 DIHYDROERGOTAMINE Ki = 1.766 nM 8.75
CHEMBL1385840 ERGOCORNINE IC50 = 3.058 nM 8.52
CHEMBL1255837 DIHYDROERGOCRISTINE MESYLATE Ki = 3.606 nM 8.44
CHEMBL629 AMITRIPTYLINE Ki = 3.687 nM 8.43
CHEMBL442 ERGOTAMINE IC50 = 3.844 nM 8.41
CHEMBL1732 DIHYDROERGOTAMINE IC50 = 3.867 nM 8.41
CHEMBL728 PROCHLORPERAZINE Ki = 4.741 nM 8.32
CHEMBL19215 METERGOLINE Ki = 7.516 nM 8.12
CHEMBL15245 YOHIMBINE Ki = 7.947 nM 8.10
CHEMBL1255837 DIHYDROERGOCRISTINE MESYLATE IC50 = 7.9 nM 8.10
CHEMBL629 AMITRIPTYLINE IC50 = 8.076 nM 8.09
CHEMBL597 PHENTOLAMINE Ki = 8.228 nM 8.09
CHEMBL564 PROMAZINE Ki = 8.418 nM 8.07
CHEMBL728 PROCHLORPERAZINE IC50 = 10.0 nM 8.00
CHEMBL42 CLOZAPINE Ki = 11.0 nM 7.96
CHEMBL1909065 MADURAMICIN ACID Ki = 12.0 nM 7.92
CHEMBL71 CHLORPROMAZINE Ki = 12.0 nM 7.92
CHEMBL85 RISPERIDONE Ki = 12.0 nM 7.92
CHEMBL1403281 ERGOCRYPTINE Ki = 12.0 nM 7.92
CHEMBL726 FLUPHENAZINE Ki = 13.0 nM 7.89
CHEMBL493 BROMOCRIPTINE Ki = 16.0 nM 7.80
CHEMBL19215 METERGOLINE IC50 = 16.0 nM 7.80
CHEMBL15245 YOHIMBINE IC50 = 17.0 nM 7.77
CHEMBL516 CYPROHEPTADINE Ki = 17.0 nM 7.77
CHEMBL564 PROMAZINE IC50 = 18.0 nM 7.75
CHEMBL597 PHENTOLAMINE IC50 = 18.0 nM 7.75
CHEMBL42 CLOZAPINE IC50 = 23.0 nM 7.64
CHEMBL643 PROMETHAZINE Ki = 24.0 nM 7.62
CHEMBL6437 MIANSERIN Ki = 24.0 nM 7.62
CHEMBL71 CHLORPROMAZINE IC50 = 26.0 nM 7.58
CHEMBL85 RISPERIDONE IC50 = 26.0 nM 7.58
CHEMBL1403281 ERGOCRYPTINE IC50 = 26.0 nM 7.58
CHEMBL1909065 MADURAMICIN ACID IC50 = 27.0 nM 7.57
CHEMBL531 PERGOLIDE Ki = 29.0 nM 7.54
CHEMBL726 FLUPHENAZINE IC50 = 29.0 nM 7.54
CHEMBL1201203 BENZTROPINE Ki = 30.0 nM 7.52
CHEMBL1628227 DOXEPIN Ki = 32.0 nM 7.50
CHEMBL493 BROMOCRIPTINE IC50 = 35.0 nM 7.46
CHEMBL134 CLONIDINE Ki = 38.0 nM 7.42
CHEMBL516 CYPROHEPTADINE IC50 = 38.0 nM 7.42
CHEMBL723 CARVEDILOL Ki = 43.0 nM 7.37
CHEMBL445 NORTRIPTYLINE Ki = 43.0 nM 7.37
CHEMBL716 QUETIAPINE Ki = 45.8 nM 7.34
CHEMBL415 CLOMIPRAMINE Ki = 46.0 nM 7.34