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Assay Detail

CHEMBL866801

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

Binding
Displacement of [3H]spiperone from human dopamine receptor D3 in CHO cell membrane
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

2-[(4-phenylpiperazin-1-yl)methyl]imidazo(di)azines as selective D4-ligands. Induction of penile erection by 2-[4-(2-methoxyphenyl)piperazin-1-ylmethyl]imidazo[1,2-a]pyridine (PIP3EA), a potent and selective D4 partial agonist.
Enguehard-Gueiffier C, Hübner H, El Hakmaoui A, Allouchi H, Gmeiner P, Argiolas A, Melis MR, Gueiffier A.
J Med Chem (2006) 49 : 3938 -3947
PubMed 16789750 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 26 5.63 6.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL208274 1 6.41
CHEMBL211590 1 6.33
CHEMBL379125 1 6.22
CHEMBL211539 1 6.17
CHEMBL211164 1 6.10
CHEMBL207543 1 6.07
CHEMBL380287 1 6.06
CHEMBL42 CLOZAPINE 4.0 1 6.02
CHEMBL212160 1 6.00
CHEMBL210341 1 6.00
CHEMBL378515 1 5.85
CHEMBL209034 1 5.82
CHEMBL378680 1 5.77
CHEMBL140099 1 5.77
CHEMBL211118 1 5.68
CHEMBL210551 1 5.62
CHEMBL380054 1 5.51
CHEMBL210283 1 5.46
CHEMBL212631 1 5.41
CHEMBL7927 FAUC 113 1 5.30
CHEMBL207488 1 5.25
CHEMBL211135 1 5.11
CHEMBL212370 1 5.06
CHEMBL143761 1 4.82
CHEMBL377542 1 4.38
CHEMBL425064 1 4.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL208274 Ki = 390.0 nM 6.41
CHEMBL211590 Ki = 470.0 nM 6.33
CHEMBL379125 Ki = 600.0 nM 6.22
CHEMBL211539 Ki = 670.0 nM 6.17
CHEMBL211164 Ki = 800.0 nM 6.10
CHEMBL207543 Ki = 850.0 nM 6.07
CHEMBL380287 Ki = 880.0 nM 6.06
CHEMBL42 CLOZAPINE Ki = 960.0 nM 6.02
CHEMBL212160 Ki = 1000.0 nM 6.00
CHEMBL210341 Ki = 1000.0 nM 6.00
CHEMBL378515 Ki = 1400.0 nM 5.85
CHEMBL209034 Ki = 1500.0 nM 5.82
CHEMBL378680 Ki = 1700.0 nM 5.77
CHEMBL140099 Ki = 1700.0 nM 5.77
CHEMBL211118 Ki = 2100.0 nM 5.68
CHEMBL210551 Ki = 2400.0 nM 5.62
CHEMBL380054 Ki = 3100.0 nM 5.51
CHEMBL210283 Ki = 3500.0 nM 5.46
CHEMBL212631 Ki = 3900.0 nM 5.41
CHEMBL7927 FAUC 113 Ki = 5000.0 nM 5.30
CHEMBL207488 Ki = 5600.0 nM 5.25
CHEMBL211135 Ki = 7700.0 nM 5.11
CHEMBL212370 Ki = 8800.0 nM 5.06
CHEMBL143761 Ki = 15000.0 nM 4.82
CHEMBL377542 Ki = 42000.0 nM 4.38
CHEMBL425064 Ki = 60000.0 nM 4.22