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Assay Detail

CHEMBL1909108

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

Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT6 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 HeLa
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 6 (CHEMBL3371)
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 6.36 8.77
Ki 871 6.70 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1909065 MADURAMICIN ACID 2.0 2 9.10
CHEMBL442 ERGOTAMINE 4.0 2 9.02
CHEMBL1201356 METHYLERGONOVINE 4.0 2 8.93
CHEMBL1732 DIHYDROERGOTAMINE 4.0 2 8.83
CHEMBL119443 ERGONOVINE 3.0 2 8.82
CHEMBL42 CLOZAPINE 4.0 2 8.30
CHEMBL157138 LISURIDE 3.0 2 8.26
CHEMBL715 OLANZAPINE 4.0 2 8.21
CHEMBL1385840 ERGOCORNINE 2 8.15
CHEMBL1403281 ERGOCRYPTINE 2 8.12
CHEMBL493 BROMOCRIPTINE 4.0 2 8.00
CHEMBL19215 METERGOLINE 2.0 2 7.89
CHEMBL531 PERGOLIDE 4.0 2 7.75
CHEMBL1255837 DIHYDROERGOCRISTINE MESYLATE 2 7.72
CHEMBL726 FLUPHENAZINE 4.0 2 7.62
CHEMBL71 CHLORPROMAZINE 4.0 2 7.58
CHEMBL479 THIORIDAZINE 4.0 2 7.48
CHEMBL1113 AMOXAPINE 4.0 2 7.46
CHEMBL1626 CLEMASTINE 4.0 2 7.44
CHEMBL6437 MIANSERIN 4.0 2 7.40
CHEMBL1909072 PIPAMAZINE 4.0 2 7.28
CHEMBL629 AMITRIPTYLINE 4.0 2 7.19
CHEMBL1065 METHYSERGIDE 4.0 2 7.12
CHEMBL415 CLOMIPRAMINE 4.0 2 6.94
CHEMBL728 PROCHLORPERAZINE 4.0 2 6.91
CHEMBL564 PROMAZINE 4.0 2 6.90
CHEMBL516 CYPROHEPTADINE 4.0 2 6.89
CHEMBL1628227 DOXEPIN 4.0 2 6.83
CHEMBL445 NORTRIPTYLINE 4.0 2 6.59
CHEMBL1255834 BW-723C86 2 6.53

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1909065 MADURAMICIN ACID Ki = 0.789 nM 9.10
CHEMBL442 ERGOTAMINE Ki = 0.948 nM 9.02
CHEMBL1201356 METHYLERGONOVINE Ki = 1.178 nM 8.93
CHEMBL1732 DIHYDROERGOTAMINE Ki = 1.486 nM 8.83
CHEMBL119443 ERGONOVINE Ki = 1.503 nM 8.82
CHEMBL1909065 MADURAMICIN ACID IC50 = 1.699 nM 8.77
CHEMBL442 ERGOTAMINE IC50 = 2.042 nM 8.69
CHEMBL1201356 METHYLERGONOVINE IC50 = 2.538 nM 8.60
CHEMBL1732 DIHYDROERGOTAMINE IC50 = 3.201 nM 8.49
CHEMBL119443 ERGONOVINE IC50 = 3.237 nM 8.49
CHEMBL42 CLOZAPINE Ki = 5.055 nM 8.30
CHEMBL157138 LISURIDE Ki = 5.514 nM 8.26
CHEMBL715 OLANZAPINE Ki = 6.109 nM 8.21
CHEMBL1385840 ERGOCORNINE Ki = 7.093 nM 8.15
CHEMBL1403281 ERGOCRYPTINE Ki = 7.559 nM 8.12
CHEMBL493 BROMOCRIPTINE Ki = 10.0 nM 8.00
CHEMBL42 CLOZAPINE IC50 = 11.0 nM 7.96
CHEMBL157138 LISURIDE IC50 = 12.0 nM 7.92
CHEMBL19215 METERGOLINE Ki = 13.0 nM 7.89
CHEMBL715 OLANZAPINE IC50 = 13.0 nM 7.89
CHEMBL1385840 ERGOCORNINE IC50 = 15.0 nM 7.82
CHEMBL1403281 ERGOCRYPTINE IC50 = 16.0 nM 7.80
CHEMBL531 PERGOLIDE Ki = 18.0 nM 7.75
CHEMBL1255837 DIHYDROERGOCRISTINE MESYLATE Ki = 19.0 nM 7.72
CHEMBL493 BROMOCRIPTINE IC50 = 22.0 nM 7.66
CHEMBL726 FLUPHENAZINE Ki = 24.0 nM 7.62
CHEMBL71 CHLORPROMAZINE Ki = 26.0 nM 7.58
CHEMBL19215 METERGOLINE IC50 = 28.0 nM 7.55
CHEMBL479 THIORIDAZINE Ki = 33.0 nM 7.48
CHEMBL1113 AMOXAPINE Ki = 35.0 nM 7.46
CHEMBL1626 CLEMASTINE Ki = 36.0 nM 7.44
CHEMBL531 PERGOLIDE IC50 = 39.0 nM 7.41
CHEMBL6437 MIANSERIN Ki = 40.0 nM 7.40
CHEMBL1255837 DIHYDROERGOCRISTINE MESYLATE IC50 = 42.0 nM 7.38
CHEMBL1909072 PIPAMAZINE Ki = 52.0 nM 7.28
CHEMBL726 FLUPHENAZINE IC50 = 52.0 nM 7.28
CHEMBL71 CHLORPROMAZINE IC50 = 57.0 nM 7.24
CHEMBL629 AMITRIPTYLINE Ki = 65.0 nM 7.19
CHEMBL479 THIORIDAZINE IC50 = 71.0 nM 7.15
CHEMBL1113 AMOXAPINE IC50 = 76.0 nM 7.12
CHEMBL1065 METHYSERGIDE Ki = 75.0 nM 7.12
CHEMBL1626 CLEMASTINE IC50 = 77.0 nM 7.11
CHEMBL6437 MIANSERIN IC50 = 85.0 nM 7.07
CHEMBL1909072 PIPAMAZINE IC50 = 112.0 nM 6.95
CHEMBL415 CLOMIPRAMINE Ki = 114.0 nM 6.94
CHEMBL728 PROCHLORPERAZINE Ki = 124.0 nM 6.91
CHEMBL564 PROMAZINE Ki = 127.0 nM 6.90
CHEMBL516 CYPROHEPTADINE Ki = 130.0 nM 6.89
CHEMBL629 AMITRIPTYLINE IC50 = 140.0 nM 6.85
CHEMBL1628227 DOXEPIN Ki = 149.0 nM 6.83