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Assay Detail

CHEMBL3366153

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

Binding
Displacement of [3H]Ketanserin from human 5-HT2A receptor by liquid scintillation counting
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 2A (CHEMBL224)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Further evaluation of the tropane analogs of haloperidol.
Sampson D, Bricker B, Zhu XY, Peprah K, Lamango NS, Setola V, Roth BL, Ablordeppey SY.
Bioorg Med Chem Lett (2014) 24 : 4294 -4297
PubMed 25070422 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 7.00 8.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL715 OLANZAPINE 4.0 1 8.48
CHEMBL210578 1 7.51
CHEMBL1940404 1 7.14
CHEMBL3321790 1 7.05
CHEMBL1940403 1 7.03
CHEMBL3321792 1 6.94
CHEMBL54 HALOPERIDOL 4.0 1 6.92
CHEMBL3321789 1 6.63
CHEMBL1940402 1 6.52
CHEMBL3321788 1 6.50
CHEMBL3321791 1 6.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL715 OLANZAPINE Ki = 3.3 nM 8.48
CHEMBL210578 Ki = 30.9 nM 7.51
CHEMBL1940404 Ki = 72.0 nM 7.14
CHEMBL3321790 Ki = 89.0 nM 7.05
CHEMBL1940403 Ki = 93.0 nM 7.03
CHEMBL3321792 Ki = 115.0 nM 6.94
CHEMBL54 HALOPERIDOL Ki = 120.0 nM 6.92
CHEMBL3321789 Ki = 236.0 nM 6.63
CHEMBL1940402 Ki = 302.0 nM 6.52
CHEMBL3321788 Ki = 317.0 nM 6.50
CHEMBL3321791 Ki = 509.0 nM 6.29