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Assay Detail

CHEMBL1909211

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

Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)
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 2A (CHEMBL224) ↗
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 6.80 9.46
Ki 871 7.34 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL85 RISPERIDONE 4.0 2 10.00
CHEMBL19215 METERGOLINE 2.0 2 9.95
CHEMBL516 CYPROHEPTADINE 4.0 2 9.56
CHEMBL1113 AMOXAPINE 4.0 2 9.35
CHEMBL6437 MIANSERIN 4.0 2 9.30
CHEMBL1909072 PIPAMAZINE 4.0 2 9.26
CHEMBL119443 ERGONOVINE 3.0 2 9.20
CHEMBL1201356 METHYLERGONOVINE 4.0 2 9.14
CHEMBL1108 DROPERIDOL 4.0 2 9.13
CHEMBL157138 LISURIDE 3.0 2 9.06
CHEMBL1729 CISAPRIDE 4.0 2 8.96
CHEMBL71 CHLORPROMAZINE 4.0 2 8.96
CHEMBL42 CLOZAPINE 4.0 2 8.92
CHEMBL479 THIORIDAZINE 4.0 2 8.90
CHEMBL715 OLANZAPINE 4.0 2 8.84
CHEMBL726 FLUPHENAZINE 4.0 2 8.84
CHEMBL442 ERGOTAMINE 4.0 2 8.73
CHEMBL728 PROCHLORPERAZINE 4.0 2 8.70
CHEMBL1732 DIHYDROERGOTAMINE 4.0 2 8.64
CHEMBL1909065 MADURAMICIN ACID 2.0 2 8.61
CHEMBL1065 METHYSERGIDE 4.0 2 8.42
CHEMBL531 PERGOLIDE 4.0 2 8.41
CHEMBL1255837 DIHYDROERGOCRISTINE MESYLATE — 2 8.37
CHEMBL629 AMITRIPTYLINE 4.0 2 8.36
CHEMBL296419 ASTEMIZOLE 4.0 2 8.25
CHEMBL621 TRAZODONE 4.0 2 8.25
CHEMBL564 PROMAZINE 4.0 2 8.17
CHEMBL1201203 BENZTROPINE 4.0 2 8.16
CHEMBL1385840 ERGOCORNINE — 2 8.10
CHEMBL534 KETOTIFEN 4.0 2 8.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL85 RISPERIDONE Ki = 0.099 nM 10.00
CHEMBL19215 METERGOLINE Ki = 0.113 nM 9.95
CHEMBL516 CYPROHEPTADINE Ki = 0.278 nM 9.56
CHEMBL85 RISPERIDONE IC50 = 0.346 nM 9.46
CHEMBL19215 METERGOLINE IC50 = 0.395 nM 9.40
CHEMBL1113 AMOXAPINE Ki = 0.444 nM 9.35
CHEMBL6437 MIANSERIN Ki = 0.504 nM 9.30
CHEMBL1909072 PIPAMAZINE Ki = 0.554 nM 9.26
CHEMBL119443 ERGONOVINE Ki = 0.63 nM 9.20
CHEMBL1201356 METHYLERGONOVINE Ki = 0.728 nM 9.14
CHEMBL1108 DROPERIDOL Ki = 0.738 nM 9.13
CHEMBL157138 LISURIDE Ki = 0.868 nM 9.06
CHEMBL516 CYPROHEPTADINE IC50 = 0.973 nM 9.01
CHEMBL71 CHLORPROMAZINE Ki = 1.1 nM 8.96
CHEMBL1729 CISAPRIDE Ki = 1.102 nM 8.96
CHEMBL42 CLOZAPINE Ki = 1.199 nM 8.92
CHEMBL479 THIORIDAZINE Ki = 1.247 nM 8.90
CHEMBL715 OLANZAPINE Ki = 1.433 nM 8.84
CHEMBL726 FLUPHENAZINE Ki = 1.458 nM 8.84
CHEMBL1113 AMOXAPINE IC50 = 1.552 nM 8.81
CHEMBL6437 MIANSERIN IC50 = 1.764 nM 8.75
CHEMBL442 ERGOTAMINE Ki = 1.853 nM 8.73
CHEMBL1909072 PIPAMAZINE IC50 = 1.938 nM 8.71
CHEMBL728 PROCHLORPERAZINE Ki = 2.018 nM 8.70
CHEMBL119443 ERGONOVINE IC50 = 2.205 nM 8.66
CHEMBL1732 DIHYDROERGOTAMINE Ki = 2.273 nM 8.64
CHEMBL1909065 MADURAMICIN ACID Ki = 2.484 nM 8.61
CHEMBL1201356 METHYLERGONOVINE IC50 = 2.547 nM 8.59
CHEMBL1108 DROPERIDOL IC50 = 2.584 nM 8.59
CHEMBL157138 LISURIDE IC50 = 3.04 nM 8.52
CHEMBL1065 METHYSERGIDE Ki = 3.832 nM 8.42
CHEMBL1729 CISAPRIDE IC50 = 3.856 nM 8.41
CHEMBL71 CHLORPROMAZINE IC50 = 3.851 nM 8.41
CHEMBL531 PERGOLIDE Ki = 3.904 nM 8.41
CHEMBL42 CLOZAPINE IC50 = 4.195 nM 8.38
CHEMBL1255837 DIHYDROERGOCRISTINE MESYLATE Ki = 4.24 nM 8.37
CHEMBL479 THIORIDAZINE IC50 = 4.366 nM 8.36
CHEMBL629 AMITRIPTYLINE Ki = 4.374 nM 8.36
CHEMBL715 OLANZAPINE IC50 = 5.016 nM 8.30
CHEMBL726 FLUPHENAZINE IC50 = 5.104 nM 8.29
CHEMBL296419 ASTEMIZOLE Ki = 5.575 nM 8.25
CHEMBL621 TRAZODONE Ki = 5.602 nM 8.25
CHEMBL442 ERGOTAMINE IC50 = 6.486 nM 8.19
CHEMBL564 PROMAZINE Ki = 6.695 nM 8.17
CHEMBL1201203 BENZTROPINE Ki = 6.968 nM 8.16
CHEMBL728 PROCHLORPERAZINE IC50 = 7.062 nM 8.15
CHEMBL1385840 ERGOCORNINE Ki = 7.995 nM 8.10
CHEMBL1732 DIHYDROERGOTAMINE IC50 = 7.955 nM 8.10
CHEMBL1909065 MADURAMICIN ACID IC50 = 8.694 nM 8.06
CHEMBL534 KETOTIFEN Ki = 8.977 nM 8.05