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Assay Detail

CHEMBL2168000

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

Binding
Displacement of [125I]IABN from human D2L receptor expressed in HEK293 cells after 60 mins by gamma counting analysis
13
Total Activities
13
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(2) dopamine receptor (CHEMBL217)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Molecular determinants of selectivity and efficacy at the dopamine D3 receptor.
Newman AH, Beuming T, Banala AK, Donthamsetti P, Pongetti K, LaBounty A, Levy B, Cao J, Michino M, Luedtke RR, Javitch JA, Shi L.
J Med Chem (2012) 55 : 6689 -6699
PubMed 22632094 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 7.14 8.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2165677 1 8.47
CHEMBL2165676 1 8.28
CHEMBL2165678 1 7.81
CHEMBL26789 1 7.69
CHEMBL125916 1 7.43
CHEMBL2165673 1 7.34
CHEMBL2165675 1 7.20
CHEMBL2165679 1 7.08
CHEMBL346692 1 6.99
CHEMBL1424807 1 6.86
CHEMBL2165674 1 6.58
CHEMBL9666 1 6.17
CHEMBL2164434 1 4.87

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2165677 Ki = 3.4 nM 8.47
CHEMBL2165676 Ki = 5.2 nM 8.28
CHEMBL2165678 Ki = 15.6 nM 7.81
CHEMBL26789 Ki = 20.6 nM 7.69
CHEMBL125916 Ki = 37.4 nM 7.43
CHEMBL2165673 Ki = 45.9 nM 7.34
CHEMBL2165675 Ki = 63.7 nM 7.20
CHEMBL2165679 Ki = 84.0 nM 7.08
CHEMBL346692 Ki = 103.0 nM 6.99
CHEMBL1424807 Ki = 137.3 nM 6.86
CHEMBL2165674 Ki = 265.0 nM 6.58
CHEMBL9666 Ki = 679.6 nM 6.17
CHEMBL2164434 Ki = 13570.0 nM 4.87