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Assay Detail

CHEMBL1909104

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

Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)
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

5-hydroxytryptamine receptor 2B (CHEMBL1833)
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 6.40 9.36
Ki 871 6.60 9.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL19215 METERGOLINE 2.0 2 9.55
CHEMBL1065 METHYSERGIDE 4.0 2 9.45
CHEMBL1201356 METHYLERGONOVINE 4.0 2 9.02
CHEMBL442 ERGOTAMINE 4.0 2 8.66
CHEMBL119443 ERGONOVINE 3.0 2 8.58
CHEMBL157138 LISURIDE 3.0 2 8.49
CHEMBL1255837 DIHYDROERGOCRISTINE MESYLATE 2 8.38
CHEMBL1732 DIHYDROERGOTAMINE 4.0 2 8.36
CHEMBL6437 MIANSERIN 4.0 2 8.33
CHEMBL493 BROMOCRIPTINE 4.0 2 8.28
CHEMBL516 CYPROHEPTADINE 4.0 2 8.22
CHEMBL1113 AMOXAPINE 4.0 2 8.18
CHEMBL1385840 ERGOCORNINE 2 8.16
CHEMBL42 CLOZAPINE 4.0 2 8.14
CHEMBL296419 ASTEMIZOLE 4.0 2 8.13
CHEMBL1403281 ERGOCRYPTINE 2 8.09
CHEMBL723 CARVEDILOL 4.0 2 7.82
CHEMBL85 RISPERIDONE 4.0 2 7.82
CHEMBL1909065 MADURAMICIN ACID 2.0 2 7.68
CHEMBL1626 CLEMASTINE 4.0 2 7.64
CHEMBL726 FLUPHENAZINE 4.0 2 7.60
CHEMBL1172 DESLORATADINE 4.0 2 7.55
CHEMBL534 KETOTIFEN 4.0 2 7.54
CHEMBL17157 TERFENADINE 4.0 2 7.52
CHEMBL1909072 PIPAMAZINE 4.0 2 7.51
CHEMBL715 OLANZAPINE 4.0 2 7.44
CHEMBL577294 2-HYDROXYPROPYL-BETA-CYCLODEXTRIN 3.0 2 7.40
CHEMBL643 PROMETHAZINE 4.0 2 7.37
CHEMBL629 AMITRIPTYLINE 4.0 2 7.35
CHEMBL15245 YOHIMBINE 3.0 2 7.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL19215 METERGOLINE Ki = 0.281 nM 9.55
CHEMBL1065 METHYSERGIDE Ki = 0.358 nM 9.45
CHEMBL19215 METERGOLINE IC50 = 0.442 nM 9.36
CHEMBL1065 METHYSERGIDE IC50 = 0.563 nM 9.25
CHEMBL1201356 METHYLERGONOVINE Ki = 0.958 nM 9.02
CHEMBL1201356 METHYLERGONOVINE IC50 = 1.505 nM 8.82
CHEMBL442 ERGOTAMINE Ki = 2.203 nM 8.66
CHEMBL119443 ERGONOVINE Ki = 2.634 nM 8.58
CHEMBL157138 LISURIDE Ki = 3.242 nM 8.49
CHEMBL442 ERGOTAMINE IC50 = 3.461 nM 8.46
CHEMBL119443 ERGONOVINE IC50 = 4.139 nM 8.38
CHEMBL1255837 DIHYDROERGOCRISTINE MESYLATE Ki = 4.201 nM 8.38
CHEMBL1732 DIHYDROERGOTAMINE Ki = 4.33 nM 8.36
CHEMBL6437 MIANSERIN Ki = 4.642 nM 8.33
CHEMBL157138 LISURIDE IC50 = 5.095 nM 8.29
CHEMBL493 BROMOCRIPTINE Ki = 5.292 nM 8.28
CHEMBL516 CYPROHEPTADINE Ki = 6.008 nM 8.22
CHEMBL1255837 DIHYDROERGOCRISTINE MESYLATE IC50 = 6.601 nM 8.18
CHEMBL1113 AMOXAPINE Ki = 6.569 nM 8.18
CHEMBL1732 DIHYDROERGOTAMINE IC50 = 6.804 nM 8.17
CHEMBL1385840 ERGOCORNINE Ki = 6.855 nM 8.16
CHEMBL42 CLOZAPINE Ki = 7.18 nM 8.14
CHEMBL6437 MIANSERIN IC50 = 7.295 nM 8.14
CHEMBL296419 ASTEMIZOLE Ki = 7.487 nM 8.13
CHEMBL1403281 ERGOCRYPTINE Ki = 8.217 nM 8.09
CHEMBL493 BROMOCRIPTINE IC50 = 8.316 nM 8.08
CHEMBL516 CYPROHEPTADINE IC50 = 9.441 nM 8.03
CHEMBL1113 AMOXAPINE IC50 = 10.0 nM 8.00
CHEMBL1385840 ERGOCORNINE IC50 = 11.0 nM 7.96
CHEMBL42 CLOZAPINE IC50 = 11.0 nM 7.96
CHEMBL296419 ASTEMIZOLE IC50 = 12.0 nM 7.92
CHEMBL1403281 ERGOCRYPTINE IC50 = 13.0 nM 7.89
CHEMBL85 RISPERIDONE Ki = 15.0 nM 7.82
CHEMBL723 CARVEDILOL Ki = 15.0 nM 7.82
CHEMBL1909065 MADURAMICIN ACID Ki = 21.0 nM 7.68
CHEMBL85 RISPERIDONE IC50 = 23.0 nM 7.64
CHEMBL723 CARVEDILOL IC50 = 23.0 nM 7.64
CHEMBL1626 CLEMASTINE Ki = 23.0 nM 7.64
CHEMBL726 FLUPHENAZINE Ki = 25.0 nM 7.60
CHEMBL1172 DESLORATADINE Ki = 28.0 nM 7.55
CHEMBL534 KETOTIFEN Ki = 29.0 nM 7.54
CHEMBL17157 TERFENADINE Ki = 30.0 nM 7.52
CHEMBL1909072 PIPAMAZINE Ki = 31.0 nM 7.51
CHEMBL1909065 MADURAMICIN ACID IC50 = 33.0 nM 7.48
CHEMBL1626 CLEMASTINE IC50 = 36.0 nM 7.44
CHEMBL715 OLANZAPINE Ki = 36.0 nM 7.44
CHEMBL726 FLUPHENAZINE IC50 = 39.0 nM 7.41
CHEMBL577294 2-HYDROXYPROPYL-BETA-CYCLODEXTRIN Ki = 40.0 nM 7.40
CHEMBL643 PROMETHAZINE Ki = 43.0 nM 7.37
CHEMBL1172 DESLORATADINE IC50 = 43.0 nM 7.37