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Assay Detail

CHEMBL673639

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Binding
In vitro affinity against Dopamine receptor D4
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 4 7.59 8.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 8.20
CHEMBL143027 1 7.68
CHEMBL42 CLOZAPINE 4.0 1 7.42
CHEMBL143022 1 7.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL Ki = 6.31 nM 8.20
CHEMBL143027 Ki = 20.89 nM 7.68
CHEMBL42 CLOZAPINE Ki = 38.02 nM 7.42
CHEMBL143022 Ki = 91.2 nM 7.04