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Assay Detail

CHEMBL617620

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Functional
Compound was evaluated for antagonism against serotonin (5-hydroxytryptamine 2B receptor ) receptor
8
Total Activities
8
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 2B (CHEMBL323)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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
Kd 8 6.21 6.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL42 CLOZAPINE 4.0 1 6.90
CHEMBL143027 1 6.61
CHEMBL142668 1 6.36
CHEMBL142316 1 6.23
CHEMBL358895 1 6.19
CHEMBL357517 1 5.74
CHEMBL143937 1 5.46
CHEMBL141600 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL42 CLOZAPINE Kd = 125.89 nM 6.90
CHEMBL143027 Kd = 245.47 nM 6.61
CHEMBL142668 Kd = 436.52 nM 6.36
CHEMBL142316 Kd = 588.84 nM 6.23
CHEMBL358895 Kd = 645.65 nM 6.19
CHEMBL357517 Kd = 1819.7 nM 5.74
CHEMBL143937 Kd = 3467.37 nM 5.46
CHEMBL141600 Kd > 100000.0 nM -