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Assay Detail

CHEMBL1026422

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

Binding
Displacement of [3H]mesulergine from human cloned 5HT2C receptor
15
Total Activities
15
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 2C (CHEMBL225)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis, binding affinity, and molecular docking analysis of new benzofuranone derivatives as potential antipsychotics.
Aranda R, Villalba K, Raviña E, Masaguer CF, Brea J, Areias F, Domínguez E, Selent J, López L, Sanz F, Pastor M, Loza MI.
J Med Chem (2008) 51 : 6085 -6094
PubMed 18783204 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 6.43 7.98

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL42 CLOZAPINE 4.0 1 7.98
CHEMBL164471 1 7.46
CHEMBL492689 1 6.61
CHEMBL159929 1 6.47
CHEMBL143027 1 6.47
CHEMBL523680 1 6.43
CHEMBL143022 1 5.81
CHEMBL516809 1 5.48
CHEMBL54 HALOPERIDOL 4.0 1 5.14
CHEMBL516944 1 -
CHEMBL493069 1 -
CHEMBL459930 1 -
CHEMBL461627 1 -
CHEMBL494702 1 -
CHEMBL494701 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL42 CLOZAPINE Ki = 10.47 nM 7.98
CHEMBL164471 Ki = 34.67 nM 7.46
CHEMBL492689 Ki = 245.47 nM 6.61
CHEMBL159929 Ki = 338.84 nM 6.47
CHEMBL143027 Ki = 338.84 nM 6.47
CHEMBL523680 Ki = 371.54 nM 6.43
CHEMBL143022 Ki = 1548.82 nM 5.81
CHEMBL516809 Ki = 3311.31 nM 5.48
CHEMBL54 HALOPERIDOL Ki = 7244.36 nM 5.14
CHEMBL516944 Ki > 10000.0 nM -
CHEMBL493069 Ki > 10000.0 nM -
CHEMBL459930 Ki > 10000.0 nM -
CHEMBL461627 Ki > 10000.0 nM -
CHEMBL494702 Ki > 10000.0 nM -
CHEMBL494701 Ki > 10000.0 nM -