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Assay Detail

CHEMBL1909209

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

Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT)
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

5-hydroxytryptamine receptor 1A (CHEMBL273) ↗
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 6.47 9.33
Ki 871 6.71 9.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL157138 LISURIDE 3.0 2 9.57
CHEMBL1732 DIHYDROERGOTAMINE 4.0 2 9.42
CHEMBL1255837 DIHYDROERGOCRISTINE MESYLATE — 2 9.38
CHEMBL442 ERGOTAMINE 4.0 2 9.35
CHEMBL1403281 ERGOCRYPTINE — 2 8.82
CHEMBL1385840 ERGOCORNINE — 2 8.75
CHEMBL1201356 METHYLERGONOVINE 4.0 2 8.63
CHEMBL493 BROMOCRIPTINE 4.0 2 8.49
CHEMBL762 OXYMETAZOLINE 4.0 2 8.49
CHEMBL723 CARVEDILOL 4.0 2 8.48
CHEMBL19215 METERGOLINE 2.0 2 8.45
CHEMBL1909065 MADURAMICIN ACID 2.0 2 8.35
CHEMBL119443 ERGONOVINE 3.0 2 8.33
CHEMBL531 PERGOLIDE 4.0 2 8.07
CHEMBL49 BUSPIRONE 4.0 2 8.03
CHEMBL117405 — — 2 7.80
CHEMBL500 PINDOLOL 4.0 2 7.57
CHEMBL1065 METHYSERGIDE 4.0 2 7.51
CHEMBL479 THIORIDAZINE 4.0 2 7.47
CHEMBL516 CYPROHEPTADINE 4.0 2 7.16
CHEMBL452861 LEVOPROPRANOLOL 2.0 2 7.15
CHEMBL15245 YOHIMBINE 3.0 2 7.14
CHEMBL1108 DROPERIDOL 4.0 2 6.86
CHEMBL27 PROPRANOLOL 4.0 2 6.86
CHEMBL357995 BOPINDOLOL 2.0 2 6.82
CHEMBL621 TRAZODONE 4.0 2 6.75
CHEMBL429 LABETALOL 4.0 2 6.65
CHEMBL42 CLOZAPINE 4.0 2 6.55
CHEMBL404849 SULOCTIDIL 4.0 2 6.51
CHEMBL19236 MOXONIDINE 4.0 2 6.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL157138 LISURIDE Ki = 0.266 nM 9.57
CHEMBL1732 DIHYDROERGOTAMINE Ki = 0.377 nM 9.42
CHEMBL1255837 DIHYDROERGOCRISTINE MESYLATE Ki = 0.412 nM 9.38
CHEMBL442 ERGOTAMINE Ki = 0.443 nM 9.35
CHEMBL157138 LISURIDE IC50 = 0.465 nM 9.33
CHEMBL1732 DIHYDROERGOTAMINE IC50 = 0.659 nM 9.18
CHEMBL1255837 DIHYDROERGOCRISTINE MESYLATE IC50 = 0.722 nM 9.14
CHEMBL442 ERGOTAMINE IC50 = 0.774 nM 9.11
CHEMBL1403281 ERGOCRYPTINE Ki = 1.503 nM 8.82
CHEMBL1385840 ERGOCORNINE Ki = 1.775 nM 8.75
CHEMBL1201356 METHYLERGONOVINE Ki = 2.326 nM 8.63
CHEMBL1403281 ERGOCRYPTINE IC50 = 2.631 nM 8.58
CHEMBL1385840 ERGOCORNINE IC50 = 3.107 nM 8.51
CHEMBL493 BROMOCRIPTINE Ki = 3.22 nM 8.49
CHEMBL762 OXYMETAZOLINE Ki = 3.208 nM 8.49
CHEMBL723 CARVEDILOL Ki = 3.338 nM 8.48
CHEMBL19215 METERGOLINE Ki = 3.528 nM 8.45
CHEMBL1201356 METHYLERGONOVINE IC50 = 4.07 nM 8.39
CHEMBL1909065 MADURAMICIN ACID Ki = 4.475 nM 8.35
CHEMBL119443 ERGONOVINE Ki = 4.643 nM 8.33
CHEMBL493 BROMOCRIPTINE IC50 = 5.635 nM 8.25
CHEMBL762 OXYMETAZOLINE IC50 = 5.613 nM 8.25
CHEMBL723 CARVEDILOL IC50 = 5.842 nM 8.23
CHEMBL19215 METERGOLINE IC50 = 6.175 nM 8.21
CHEMBL1909065 MADURAMICIN ACID IC50 = 7.831 nM 8.11
CHEMBL119443 ERGONOVINE IC50 = 8.126 nM 8.09
CHEMBL531 PERGOLIDE Ki = 8.468 nM 8.07
CHEMBL49 BUSPIRONE Ki = 9.307 nM 8.03
CHEMBL531 PERGOLIDE IC50 = 15.0 nM 7.82
CHEMBL49 BUSPIRONE IC50 = 16.0 nM 7.80
CHEMBL117405 — Ki = 16.0 nM 7.80
CHEMBL500 PINDOLOL Ki = 27.0 nM 7.57
CHEMBL117405 — IC50 = 28.0 nM 7.55
CHEMBL1065 METHYSERGIDE Ki = 31.0 nM 7.51
CHEMBL479 THIORIDAZINE Ki = 34.0 nM 7.47
CHEMBL500 PINDOLOL IC50 = 48.0 nM 7.32
CHEMBL1065 METHYSERGIDE IC50 = 54.0 nM 7.27
CHEMBL479 THIORIDAZINE IC50 = 60.0 nM 7.22
CHEMBL516 CYPROHEPTADINE Ki = 70.0 nM 7.16
CHEMBL452861 LEVOPROPRANOLOL Ki = 71.0 nM 7.15
CHEMBL15245 YOHIMBINE Ki = 72.0 nM 7.14
CHEMBL516 CYPROHEPTADINE IC50 = 122.0 nM 6.91
CHEMBL452861 LEVOPROPRANOLOL IC50 = 124.0 nM 6.91
CHEMBL15245 YOHIMBINE IC50 = 126.0 nM 6.90
CHEMBL27 PROPRANOLOL Ki = 139.0 nM 6.86
CHEMBL1108 DROPERIDOL Ki = 138.0 nM 6.86
CHEMBL357995 BOPINDOLOL Ki = 153.0 nM 6.82
CHEMBL621 TRAZODONE Ki = 178.0 nM 6.75
CHEMBL429 LABETALOL Ki = 225.0 nM 6.65
CHEMBL1108 DROPERIDOL IC50 = 242.0 nM 6.62