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Assay Detail

CHEMBL4361372

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

Binding
Displacement of [3H]-(R)-(+)-7-OH-DPAT from recombinant human D3 receptor expressed in HEK293 cell membranes measured after 90 mins by microbeta scintillation counting analysis
37
Total Activities
31
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

The Significance of Chirality in Drug Design and Synthesis of Bitopic Ligands as D3 Receptor (D3R) Selective Agonists.
Battiti FO, Cemaj SL, Guerrero AM, Shaik AB, Lam J, Rais R, Slusher BS, Deschamps JR, Imler GH, Newman AH, Bonifazi A.
J Med Chem (2019) 62 : 6287 -6314
PubMed 31257877 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 37 6.18 8.88

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL301265 PRAMIPEXOLE 4.0 1 8.88
CHEMBL70565 1 8.77
CHEMBL4551160 1 8.73
CHEMBL4471817 1 8.62
CHEMBL4452064 1 8.22
CHEMBL4435946 1 7.51
CHEMBL4551518 1 7.39
CHEMBL4443441 1 6.76
CHEMBL4464060 1 6.73
CHEMBL4455770 4 6.56
CHEMBL4437740 1 6.55
CHEMBL4525362 1 6.55
CHEMBL4467736 2 6.45
CHEMBL4565132 1 6.39
CHEMBL4453200 1 6.37
CHEMBL4519520 1 6.21
CHEMBL4451708 1 6.09
CHEMBL4589785 1 5.94
CHEMBL4447227 1 5.92
CHEMBL4460452 1 5.88
CHEMBL4586223 1 5.82
CHEMBL4568693 1 5.80
CHEMBL4474113 1 5.67
CHEMBL4465109 1 5.22
CHEMBL4458742 1 5.19
CHEMBL4528479 1 5.06
CHEMBL4474048 1 4.95
CHEMBL4562186 1 4.68
CHEMBL4452139 1 4.62
CHEMBL4451063 3 4.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL301265 PRAMIPEXOLE Ki = 1.32 nM 8.88
CHEMBL70565 Ki = 1.69 nM 8.77
CHEMBL4551160 Ki = 1.85 nM 8.73
CHEMBL4471817 Ki = 2.42 nM 8.62
CHEMBL4452064 Ki = 5.96 nM 8.22
CHEMBL4435946 Ki = 31.2 nM 7.51
CHEMBL4551518 Ki = 40.9 nM 7.39
CHEMBL4443441 Ki = 173.0 nM 6.76
CHEMBL4464060 Ki = 185.0 nM 6.73
CHEMBL4455770 Ki = 276.0 nM 6.56
CHEMBL4437740 Ki = 282.0 nM 6.55
CHEMBL4525362 Ki = 284.0 nM 6.55
CHEMBL4467736 Ki = 354.0 nM 6.45
CHEMBL4565132 Ki = 403.0 nM 6.39
CHEMBL4455770 Ki = 404.0 nM 6.39
CHEMBL4453200 Ki = 424.0 nM 6.37
CHEMBL4519520 Ki = 613.0 nM 6.21
CHEMBL4451708 Ki = 806.0 nM 6.09
CHEMBL4589785 Ki = 1150.0 nM 5.94
CHEMBL4455770 Ki = 1190.0 nM 5.92
CHEMBL4447227 Ki = 1190.0 nM 5.92
CHEMBL4460452 Ki = 1330.0 nM 5.88
CHEMBL4586223 Ki = 1520.0 nM 5.82
CHEMBL4568693 Ki = 1590.0 nM 5.80
CHEMBL4467736 Ki = 1770.0 nM 5.75
CHEMBL4455770 Ki = 2150.0 nM 5.67
CHEMBL4474113 Ki = 2130.0 nM 5.67
CHEMBL4465109 Ki = 6010.0 nM 5.22
CHEMBL4458742 Ki = 6470.0 nM 5.19
CHEMBL4528479 Ki = 8660.0 nM 5.06
CHEMBL4474048 Ki = 11300.0 nM 4.95
CHEMBL4562186 Ki = 21100.0 nM 4.68
CHEMBL4452139 Ki = 24200.0 nM 4.62
CHEMBL4451063 Ki = 26200.0 nM 4.58
CHEMBL4451063 Ki = 32900.0 nM 4.48
CHEMBL4451063 Ki = 66200.0 nM 4.18
CHEMBL4436589 Ki = 73000.0 nM 4.14