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Assay Detail

CHEMBL3106137

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

Binding
Displacement of [3H]Ketanserin from 5-HT2A receptor (unknown origin)
10
Total Activities
5
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

The synthesis and comparative receptor binding affinities of novel, isomeric pyridoindolobenzazepine scaffolds.
Rajagopalan R, Bandyopadhyaya A, Rajagopalan DR, Rajagopalan P.
Bioorg Med Chem Lett (2014) 24 : 576 -579
PubMed 24365159 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 7.34 8.23

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL71 CHLORPROMAZINE 4.0 2 8.23
CHEMBL42 CLOZAPINE 4.0 2 8.14
CHEMBL3104091 2 7.62
CHEMBL3104093 2 6.59
CHEMBL3104092 2 6.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL71 CHLORPROMAZINE Ki = 5.888 nM 8.23
CHEMBL71 CHLORPROMAZINE Ki = 5.9 nM 8.23
CHEMBL42 CLOZAPINE Ki = 7.3 nM 8.14
CHEMBL42 CLOZAPINE Ki = 7.413 nM 8.13
CHEMBL3104091 Ki = 24.0 nM 7.62
CHEMBL3104091 Ki = 23.99 nM 7.62
CHEMBL3104093 Ki = 257.0 nM 6.59
CHEMBL3104093 Ki = 257.04 nM 6.59
CHEMBL3104092 Ki = 736.0 nM 6.13
CHEMBL3104092 Ki = 741.31 nM 6.13