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Assay Detail

CHEMBL895648

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

Binding
Displacement of [125I]IABN from human dopamine D2 receptor expressed in HEK293 cells
23
Total Activities
23
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 Expert

Target

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

Publication

Heterocyclic analogues of N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)arylcarboxamides with functionalized linking chains as novel dopamine D3 receptor ligands: potential substance abuse therapeutic agents.
Grundt P, Prevatt KM, Cao J, Taylor M, Floresca CZ, Choi JK, Jenkins BG, Luedtke RR, Newman AH.
J Med Chem (2007) 50 : 4135 -4146
PubMed 17672446 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 23 7.00 7.63

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL244562 1 7.63
CHEMBL69451 1 7.61
CHEMBL244774 1 7.59
CHEMBL390253 1 7.55
CHEMBL241973 1 7.55
CHEMBL244989 1 7.32
CHEMBL231156 1 7.27
CHEMBL110365 1 7.26
CHEMBL231055 1 7.17
CHEMBL394541 1 7.16
CHEMBL394862 1 7.08
CHEMBL244773 1 7.04
CHEMBL180010 1 7.03
CHEMBL398175 1 6.98
CHEMBL300780 1 6.95
CHEMBL242434 1 6.87
CHEMBL304605 1 6.78
CHEMBL242218 1 6.60
CHEMBL244990 1 6.57
CHEMBL242644 1 6.55
CHEMBL396024 1 6.50
CHEMBL394863 1 5.98
CHEMBL244775 1 5.94

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL244562 Ki = 23.6 nM 7.63
CHEMBL69451 Ki = 24.8 nM 7.61
CHEMBL244774 Ki = 25.8 nM 7.59
CHEMBL390253 Ki = 28.4 nM 7.55
CHEMBL241973 Ki = 28.3 nM 7.55
CHEMBL244989 Ki = 48.4 nM 7.32
CHEMBL231156 Ki = 53.7 nM 7.27
CHEMBL110365 Ki = 55.4 nM 7.26
CHEMBL231055 Ki = 68.4 nM 7.17
CHEMBL394541 Ki = 69.0 nM 7.16
CHEMBL394862 Ki = 84.0 nM 7.08
CHEMBL244773 Ki = 92.0 nM 7.04
CHEMBL180010 Ki = 93.3 nM 7.03
CHEMBL398175 Ki = 105.0 nM 6.98
CHEMBL300780 Ki = 112.0 nM 6.95
CHEMBL242434 Ki = 134.0 nM 6.87
CHEMBL304605 Ki = 168.0 nM 6.78
CHEMBL242218 Ki = 249.0 nM 6.60
CHEMBL244990 Ki = 267.0 nM 6.57
CHEMBL242644 Ki = 284.0 nM 6.55
CHEMBL396024 Ki = 319.0 nM 6.50
CHEMBL394863 Ki = 1050.0 nM 5.98
CHEMBL244775 Ki = 1160.0 nM 5.94