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

CHEMBL4052937

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

Binding
Displacement of [3H]-N-methylspiperone from human dopamine D3 receptor expressed in HEK293 cells after 1 hr by MicroBeta microplate counting method
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

D(3) dopamine receptor (CHEMBL234)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Toward Understanding the Structural Basis of Partial Agonism at the Dopamine D3 Receptor.
Michino M, Boateng CA, Donthamsetti P, Yano H, Bakare OM, Bonifazi A, Ellenberger MP, Keck TM, Kumar V, Zhu C, Verma R, Deschamps JR, Javitch JA, Newman AH, Shi L.
J Med Chem (2017) 60 : 580 -593
PubMed 27983845 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 8.03 9.76

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4093656 1 9.76
CHEMBL1627306 1 8.95
CHEMBL346692 1 8.85
CHEMBL2165677 1 8.72
CHEMBL4081424 1 8.38
CHEMBL3589651 1 8.37
CHEMBL1627307 1 7.78
CHEMBL4105681 1 7.63
CHEMBL4092928 1 7.46
CHEMBL4085184 1 7.12
CHEMBL4072171 1 6.92
CHEMBL4063564 1 6.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4093656 Ki = 0.172 nM 9.76
CHEMBL1627306 Ki = 1.12 nM 8.95
CHEMBL346692 Ki = 1.4 nM 8.85
CHEMBL2165677 Ki = 1.9 nM 8.72
CHEMBL4081424 Ki = 4.12 nM 8.38
CHEMBL3589651 Ki = 4.26 nM 8.37
CHEMBL1627307 Ki = 16.6 nM 7.78
CHEMBL4105681 Ki = 23.4 nM 7.63
CHEMBL4092928 Ki = 34.3 nM 7.46
CHEMBL4085184 Ki = 75.2 nM 7.12
CHEMBL4072171 Ki = 119.0 nM 6.92
CHEMBL4063564 Ki = 373.0 nM 6.43