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Assay Detail

CHEMBL907459

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

Binding
Displacement of [3H]ketanserin from rat cortex 5HT2A receptor
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 2A (CHEMBL322)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Towards a new generation of potential antipsychotic agents combining D2 and 5-HT1A receptor activities.
Cuisiat S, Bourdiol N, Lacharme V, Newman-Tancredi A, Colpaert F, Vacher B.
J Med Chem (2007) 50 : 865 -876
PubMed 17300168 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 6.31 7.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 7.08
CHEMBL219111 1 6.96
CHEMBL221743 1 6.72
CHEMBL413777 1 6.52
CHEMBL386988 1 6.46
CHEMBL376634 1 6.43
CHEMBL425810 1 6.25
CHEMBL220809 1 6.19
CHEMBL221692 ADOPRAZINE 2.0 1 6.14
CHEMBL218217 1 6.14
CHEMBL221957 1 5.98
CHEMBL220808 SARIZOTAN 3.0 1 5.67
CHEMBL218166 BIFEPRUNOX 3.0 1 5.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL Ki = 83.18 nM 7.08
CHEMBL219111 Ki = 109.65 nM 6.96
CHEMBL221743 Ki = 190.55 nM 6.72
CHEMBL413777 Ki = 302.0 nM 6.52
CHEMBL386988 Ki = 346.74 nM 6.46
CHEMBL376634 Ki = 371.54 nM 6.43
CHEMBL425810 Ki = 562.34 nM 6.25
CHEMBL220809 Ki = 645.65 nM 6.19
CHEMBL221692 ADOPRAZINE Ki = 724.44 nM 6.14
CHEMBL218217 Ki = 724.44 nM 6.14
CHEMBL221957 Ki = 1047.13 nM 5.98
CHEMBL220808 SARIZOTAN Ki = 2137.96 nM 5.67
CHEMBL218166 BIFEPRUNOX Ki = 3311.31 nM 5.48