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Assay Detail

CHEMBL617039

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

Binding
Binding affinity towards 5-hydroxytryptamine 2 receptor expressed in CHO cell membranes using [3H]ketanserin (60 Ci/mmol, 1 nM)
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Serotonin 2 (5-HT2) receptor (CHEMBL2095200)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Novel indolodioxanes with antihypertensive effects: potent ligands for the 5-HT1A receptor.
Ennis MD, Baze ME, Smith MW, Lawson CF, McCall RB, Lahti RA, Piercey MF.
J Med Chem (1992) 35 : 3058 -3066
PubMed 1323682 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 7.05 7.56

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL103983 1 7.56
CHEMBL418802 1 7.50
CHEMBL318374 1 7.41
CHEMBL102175 1 7.03
CHEMBL318166 1 6.84
CHEMBL319023 1 6.77
CHEMBL101483 1 6.77
CHEMBL101535 1 6.55
CHEMBL320880 1 -
CHEMBL323088 1 -
CHEMBL106283 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL103983 Ki = 27.6 nM 7.56
CHEMBL418802 Ki = 31.6 nM 7.50
CHEMBL318374 Ki = 38.7 nM 7.41
CHEMBL102175 Ki = 92.6 nM 7.03
CHEMBL318166 Ki = 143.0 nM 6.84
CHEMBL319023 Ki = 170.0 nM 6.77
CHEMBL101483 Ki = 171.0 nM 6.77
CHEMBL101535 Ki = 281.0 nM 6.55
CHEMBL320880 Ki > 1722.0 nM -
CHEMBL323088 Ki > 1722.0 nM -
CHEMBL106283 Ki > 1722.0 nM -