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Assay Detail

CHEMBL4000277

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

Binding
Displacement of [3H]-raclopride from human dopamine D2L receptor expressed in F1pIn CHO cells after 60 mins by scintillation counting analysis
12
Total Activities
6
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

D(2) dopamine receptor (CHEMBL217)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Proof of concept study for designed multiple ligands targeting the dopamine D2, serotonin 5-HT2A, and muscarinic M1 acetylcholine receptors.
Szabo M, Lim HD, Herenbrink CK, Christopoulos A, Lane JR, Capuano B.
J Med Chem (2015) 58 : 1550 -1555
PubMed 25590655 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 7.50 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4104013 2 8.77
CHEMBL4062602 2 8.49
CHEMBL4090568 2 7.75
CHEMBL4066435 2 7.37
CHEMBL4093980 2 6.56
CHEMBL1242923 2 6.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4104013 Ki = 1.7 nM 8.77
CHEMBL4104013 Ki = 1.738 nM 8.76
CHEMBL4062602 Ki = 3.236 nM 8.49
CHEMBL4062602 Ki = 3.2 nM 8.49
CHEMBL4090568 Ki = 17.78 nM 7.75
CHEMBL4090568 Ki = 17.7 nM 7.75
CHEMBL4066435 Ki = 42.66 nM 7.37
CHEMBL4066435 Ki = 42.7 nM 7.37
CHEMBL4093980 Ki = 275.42 nM 6.56
CHEMBL4093980 Ki = 273.0 nM 6.56
CHEMBL1242923 Ki = 831.76 nM 6.08
CHEMBL1242923 Ki = 834.0 nM 6.08