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Assay Detail

CHEMBL2167671

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Functional
Antagonist activity at 5HT2A receptor
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Life beyond kinases: structure-based discovery of sorafenib as nanomolar antagonist of 5-HT receptors.
Lin X, Huang XP, Chen G, Whaley R, Peng S, Wang Y, Zhang G, Wang SX, Wang S, Roth BL, Huang N.
J Med Chem (2012) 55 : 5749 -5759
PubMed 22694093 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 9.02 9.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL516 CYPROHEPTADINE 4.0 1 9.34
CHEMBL51 KETANSERIN 3.0 1 8.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL516 CYPROHEPTADINE Ki = 0.46 nM 9.34
CHEMBL51 KETANSERIN Ki = 2.0 nM 8.70