Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL670970

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

Binding
Affinity against Dopamine receptor D2
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

D(2) dopamine receptor (CHEMBL339)
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
Ki 11 7.10 8.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54 HALOPERIDOL 4.0 1 8.48
CHEMBL85 RISPERIDONE 4.0 1 8.09
CHEMBL143027 1 8.02
CHEMBL143022 1 7.02
CHEMBL42 CLOZAPINE 4.0 1 6.58
CHEMBL142668 1 6.39
CHEMBL357517 1 5.14
CHEMBL358895 1 -
CHEMBL142316 1 -
CHEMBL143937 1 -
CHEMBL141600 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54 HALOPERIDOL Ki = 3.311 nM 8.48
CHEMBL85 RISPERIDONE Ki = 8.128 nM 8.09
CHEMBL143027 Ki = 9.55 nM 8.02
CHEMBL143022 Ki = 95.5 nM 7.02
CHEMBL42 CLOZAPINE Ki = 263.03 nM 6.58
CHEMBL142668 Ki = 407.38 nM 6.39
CHEMBL357517 Ki = 7244.36 nM 5.14
CHEMBL358895 Ki < 10000.0 nM -
CHEMBL142316 Ki < 10000.0 nM -
CHEMBL143937 Ki < 10000.0 nM -
CHEMBL141600 Ki < 10000.0 nM -