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Assay Detail

CHEMBL617695

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

Binding
Affinity at 5-hydroxytryptamine 2A receptor of the rat brain cortex was assessed on the basis of their ability to displace [3H]ketanserin
10
Total Activities
10
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

Application of similarity matrices and genetic neural networks in quantitative structure-activity relationships of 2- or 4-(4-Methylpiperazino)pyrimidines: 5-HT(2A) receptor antagonists.
Borowski T, Król M, Broclawik E, Baranowski TC, Strekowski L, Mokrosz MJ.
J Med Chem (2000) 43 : 1901 -1909
PubMed 10821703 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 6.65 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL42 CLOZAPINE 4.0 1 8.80
CHEMBL43163 1 8.10
CHEMBL289064 1 8.00
CHEMBL43486 1 7.30
CHEMBL42261 1 6.68
CHEMBL57027 1 6.46
CHEMBL56931 1 5.57
CHEMBL56116 1 5.37
CHEMBL56224 1 5.22
CHEMBL56384 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL42 CLOZAPINE Ki = 1.585 nM 8.80
CHEMBL43163 Ki = 7.943 nM 8.10
CHEMBL289064 Ki = 10.0 nM 8.00
CHEMBL43486 Ki = 50.12 nM 7.30
CHEMBL42261 Ki = 208.93 nM 6.68
CHEMBL57027 Ki = 346.74 nM 6.46
CHEMBL56931 Ki = 2691.53 nM 5.57
CHEMBL56116 Ki = 4265.8 nM 5.37
CHEMBL56224 Ki = 6025.6 nM 5.22
CHEMBL56384 Ki = 10000.0 nM 5.00