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Assay Detail

CHEMBL617647

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Binding
In vitro affinity against serotonin (5-hydroxytryptamine 2C) receptor
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 2C (CHEMBL225)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Conformationally constrained butyrophenones with affinity for dopamine (D(1), D(2), D(4)) and serotonin (5-HT(2A), 5-HT(2B), 5-HT(2C)) receptors: synthesis of aminomethylbenzo[b]furanones and their evaluation as antipsychotics.
Raviña E, Casariego I, Masaguer CF, Fontenla JA, Montenegro GY, Rivas ME, Loza MI, Enguix MJ, Villazon M, Cadavid MI, Demontis GC.
J Med Chem (2000) 43 : 4678 -4693
PubMed 11101359 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 6.24 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL42 CLOZAPINE 4.0 1 8.30
CHEMBL85 RISPERIDONE 4.0 1 7.38
CHEMBL143937 1 6.64
CHEMBL141600 1 5.47
CHEMBL358895 1 4.89
CHEMBL143027 1 4.74
CHEMBL357517 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL42 CLOZAPINE Ki = 5.012 nM 8.30
CHEMBL85 RISPERIDONE Ki = 41.69 nM 7.38
CHEMBL143937 Ki = 229.09 nM 6.64
CHEMBL141600 Ki = 3388.44 nM 5.47
CHEMBL358895 Ki = 12882.5 nM 4.89
CHEMBL143027 Ki = 18197.01 nM 4.74
CHEMBL357517 Ki < 100000.0 nM -