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Assay Detail

CHEMBL3599874

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 (unknown origin) expressed in HEK293 cells after 1 hr by liquid scintillation counting
25
Total Activities
25
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

High Affinity Dopamine D3 Receptor (D3R)-Selective Antagonists Attenuate Heroin Self-Administration in Wild-Type but not D3R Knockout Mice.
Boateng CA, Bakare OM, Zhan J, Banala AK, Burzynski C, Pommier E, Keck TM, Donthamsetti P, Javitch JA, Rais R, Slusher BS, Xi ZX, Newman AH.
J Med Chem (2015) 58 : 6195 -6213
PubMed 26203768 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 25 8.51 9.93

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3597643 1 9.93
CHEMBL3597645 1 9.89
CHEMBL3597644 1 9.76
CHEMBL3596212 1 9.61
CHEMBL68740 1 9.55
CHEMBL3597635 1 9.46
CHEMBL3597641 1 9.41
CHEMBL3597639 1 9.24
CHEMBL3597642 1 9.04
CHEMBL1627310 1 8.74
CHEMBL1627305 1 8.73
CHEMBL3597637 1 8.70
CHEMBL3597650 1 8.67
CHEMBL3597647 1 8.60
CHEMBL127317 1 8.46
CHEMBL3597636 1 8.44
CHEMBL3597640 1 8.09
CHEMBL3597638 1 7.50
CHEMBL3597649 1 7.47
CHEMBL3597654 1 7.42
CHEMBL3597651 1 7.35
CHEMBL3597652 1 7.28
CHEMBL3597648 1 7.28
CHEMBL3597653 1 7.16
CHEMBL3597646 1 7.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3597643 Ki = 0.118 nM 9.93
CHEMBL3597645 Ki = 0.128 nM 9.89
CHEMBL3597644 Ki = 0.173 nM 9.76
CHEMBL3596212 Ki = 0.244 nM 9.61
CHEMBL68740 Ki = 0.28 nM 9.55
CHEMBL3597635 Ki = 0.351 nM 9.46
CHEMBL3597641 Ki = 0.392 nM 9.41
CHEMBL3597639 Ki = 0.57 nM 9.24
CHEMBL3597642 Ki = 0.907 nM 9.04
CHEMBL1627310 Ki = 1.8 nM 8.74
CHEMBL1627305 Ki = 1.88 nM 8.73
CHEMBL3597637 Ki = 1.99 nM 8.70
CHEMBL3597650 Ki = 2.14 nM 8.67
CHEMBL3597647 Ki = 2.51 nM 8.60
CHEMBL127317 Ki = 3.46 nM 8.46
CHEMBL3597636 Ki = 3.63 nM 8.44
CHEMBL3597640 Ki = 8.05 nM 8.09
CHEMBL3597638 Ki = 31.6 nM 7.50
CHEMBL3597649 Ki = 33.8 nM 7.47
CHEMBL3597654 Ki = 37.7 nM 7.42
CHEMBL3597651 Ki = 44.8 nM 7.35
CHEMBL3597652 Ki = 52.9 nM 7.28
CHEMBL3597648 Ki = 53.1 nM 7.28
CHEMBL3597653 Ki = 69.9 nM 7.16
CHEMBL3597646 Ki = 97.9 nM 7.01