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Assay Detail

CHEMBL1909210

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

Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
1742
Total Activities
871
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 1B (CHEMBL3459)
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 6.36 9.70
Ki 871 6.67 10.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL442 ERGOTAMINE 4.0 2 10.04
CHEMBL1732 DIHYDROERGOTAMINE 4.0 2 9.42
CHEMBL762 OXYMETAZOLINE 4.0 2 9.04
CHEMBL119443 ERGONOVINE 3.0 2 8.89
CHEMBL1909065 MADURAMICIN ACID 2.0 2 8.87
CHEMBL157138 LISURIDE 3.0 2 8.34
CHEMBL1403281 ERGOCRYPTINE 2 8.30
CHEMBL128 SUMATRIPTAN 4.0 2 8.09
CHEMBL1201356 METHYLERGONOVINE 4.0 2 8.03
CHEMBL1255837 DIHYDROERGOCRISTINE MESYLATE 2 7.96
CHEMBL19215 METERGOLINE 2.0 2 7.96
CHEMBL1385840 ERGOCORNINE 2 7.72
CHEMBL531 PERGOLIDE 4.0 2 7.40
CHEMBL493 BROMOCRIPTINE 4.0 2 7.33
CHEMBL1065 METHYSERGIDE 4.0 2 6.97
CHEMBL1626 CLEMASTINE 4.0 2 6.66
CHEMBL1255834 BW-723C86 2 6.40
CHEMBL715 OLANZAPINE 4.0 2 6.36
CHEMBL723 CARVEDILOL 4.0 2 6.23
CHEMBL296419 ASTEMIZOLE 4.0 2 6.20
CHEMBL621 TRAZODONE 4.0 2 6.08
CHEMBL81 RALOXIFENE 4.0 2 6.07
CHEMBL726 FLUPHENAZINE 4.0 2 6.06
CHEMBL42 CLOZAPINE 4.0 2 6.02
CHEMBL728 PROCHLORPERAZINE 4.0 2 5.92
CHEMBL516 CYPROHEPTADINE 4.0 2 5.90
CHEMBL1200558 BACITRACIN 4.0 2 5.87
CHEMBL1909072 PIPAMAZINE 4.0 2 5.86
CHEMBL305660 EBASTINE 4.0 2 5.85
CHEMBL445 NORTRIPTYLINE 4.0 2 5.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL442 ERGOTAMINE Ki = 0.091 nM 10.04
CHEMBL442 ERGOTAMINE IC50 = 0.201 nM 9.70
CHEMBL1732 DIHYDROERGOTAMINE Ki = 0.384 nM 9.42
CHEMBL1732 DIHYDROERGOTAMINE IC50 = 0.846 nM 9.07
CHEMBL762 OXYMETAZOLINE Ki = 0.909 nM 9.04
CHEMBL119443 ERGONOVINE Ki = 1.293 nM 8.89
CHEMBL1909065 MADURAMICIN ACID Ki = 1.353 nM 8.87
CHEMBL762 OXYMETAZOLINE IC50 = 2.0 nM 8.70
CHEMBL119443 ERGONOVINE IC50 = 2.845 nM 8.55
CHEMBL1909065 MADURAMICIN ACID IC50 = 2.977 nM 8.53
CHEMBL157138 LISURIDE Ki = 4.594 nM 8.34
CHEMBL1403281 ERGOCRYPTINE Ki = 5.021 nM 8.30
CHEMBL1403281 ERGOCRYPTINE IC50 = 8.199 nM 8.09
CHEMBL128 SUMATRIPTAN Ki = 8.191 nM 8.09
CHEMBL1201356 METHYLERGONOVINE Ki = 9.263 nM 8.03
CHEMBL157138 LISURIDE IC50 = 10.0 nM 8.00
CHEMBL1255837 DIHYDROERGOCRISTINE MESYLATE Ki = 11.0 nM 7.96
CHEMBL19215 METERGOLINE Ki = 11.0 nM 7.96
CHEMBL1201356 METHYLERGONOVINE IC50 = 15.0 nM 7.82
CHEMBL128 SUMATRIPTAN IC50 = 18.0 nM 7.75
CHEMBL1385840 ERGOCORNINE Ki = 19.0 nM 7.72
CHEMBL19215 METERGOLINE IC50 = 19.0 nM 7.72
CHEMBL1255837 DIHYDROERGOCRISTINE MESYLATE IC50 = 24.0 nM 7.62
CHEMBL1385840 ERGOCORNINE IC50 = 30.0 nM 7.52
CHEMBL531 PERGOLIDE Ki = 40.0 nM 7.40
CHEMBL493 BROMOCRIPTINE Ki = 47.0 nM 7.33
CHEMBL531 PERGOLIDE IC50 = 87.0 nM 7.06
CHEMBL493 BROMOCRIPTINE IC50 = 103.0 nM 6.99
CHEMBL1065 METHYSERGIDE Ki = 108.0 nM 6.97
CHEMBL1065 METHYSERGIDE IC50 = 177.0 nM 6.75
CHEMBL1626 CLEMASTINE Ki = 220.0 nM 6.66
CHEMBL1626 CLEMASTINE IC50 = 359.0 nM 6.45
CHEMBL1255834 BW-723C86 Ki = 400.1 nM 6.40
CHEMBL1255834 BW-723C86 IC50 = 421.1 nM 6.38
CHEMBL715 OLANZAPINE Ki = 433.0 nM 6.36
CHEMBL723 CARVEDILOL Ki = 589.0 nM 6.23
CHEMBL296419 ASTEMIZOLE Ki = 630.0 nM 6.20
CHEMBL715 OLANZAPINE IC50 = 707.0 nM 6.15
CHEMBL621 TRAZODONE Ki = 830.0 nM 6.08
CHEMBL81 RALOXIFENE Ki = 846.0 nM 6.07
CHEMBL726 FLUPHENAZINE Ki = 869.0 nM 6.06
CHEMBL42 CLOZAPINE Ki = 959.0 nM 6.02
CHEMBL728 PROCHLORPERAZINE Ki = 1205.0 nM 5.92
CHEMBL516 CYPROHEPTADINE Ki = 1263.0 nM 5.90
CHEMBL723 CARVEDILOL IC50 = 1295.0 nM 5.89
CHEMBL621 TRAZODONE IC50 = 1356.0 nM 5.87
CHEMBL1200558 BACITRACIN Ki = 1354.0 nM 5.87
CHEMBL1909072 PIPAMAZINE Ki = 1367.0 nM 5.86
CHEMBL296419 ASTEMIZOLE IC50 = 1387.0 nM 5.86
CHEMBL305660 EBASTINE Ki = 1417.1 nM 5.85