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Assay Detail

CHEMBL954230

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

Binding
Displacement of [3H]ketanserin from rat 5HT2A receptor expressed in mouse NIH3T3 cells
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type NIH3T3
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

'Hybrid' benzofuran-benzopyran congeners as rigid analogs of hallucinogenic phenethylamines.
Schultz DM, Prescher JA, Kidd S, Marona-Lewicka D, Nichols DE, Monte A.
Bioorg Med Chem (2008) 16 : 6242 -6251
PubMed 18467103 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 8.39 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL520449 1 9.00
CHEMBL101008 1 9.00
CHEMBL482702 1 8.51
CHEMBL519145 1 8.44
CHEMBL482675 1 8.35
CHEMBL520133 1 8.28
CHEMBL482704 1 8.08
CHEMBL482703 1 7.96
CHEMBL6607 BROLAMFETAMINE 2.0 1 7.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL520449 Ki = 1.0 nM 9.00
CHEMBL101008 Ki = 1.0 nM 9.00
CHEMBL482702 Ki = 3.1 nM 8.51
CHEMBL519145 Ki = 3.6 nM 8.44
CHEMBL482675 Ki = 4.5 nM 8.35
CHEMBL520133 Ki = 5.3 nM 8.28
CHEMBL482704 Ki = 8.4 nM 8.08
CHEMBL482703 Ki = 11.0 nM 7.96
CHEMBL6607 BROLAMFETAMINE Ki = 13.0 nM 7.89