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Assay Detail

CHEMBL672374

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

Binding
Ability to bind to Dopamine receptor D2 in vitro in rat sriatal membranes using [3H]spiperone radioligand
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

D(2) dopamine receptor (CHEMBL339)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

New arylpiperazine 5-HT(1A) receptor ligands containing the pyrimido[2,1-f]purine fragment: synthesis, in vitro, and in vivo pharmacological evaluation.
Jurczyk S, Kołaczkowski M, Maryniak E, Zajdel P, Pawłowski M, Tatarczyńska E, Kłodzińska A, Chojnacka-Wójcik E, Bojarski AJ, Charakchieva-Minol S, Duszyńska B, Nowak G, Maciag D.
J Med Chem (2004) 47 : 2659 -2666
PubMed 15115407 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 6.43 7.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL191907 1 7.03
CHEMBL2112359 1 6.78
CHEMBL2112351 1 6.74
CHEMBL2112361 1 6.65
CHEMBL195849 1 6.58
CHEMBL193867 1 6.49
CHEMBL195047 1 6.38
CHEMBL193595 1 6.37
CHEMBL425567 1 5.93
CHEMBL2112362 1 5.91
CHEMBL2112360 1 5.88

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL191907 Ki = 94.0 nM 7.03
CHEMBL2112359 Ki = 165.0 nM 6.78
CHEMBL2112351 Ki = 182.0 nM 6.74
CHEMBL2112361 Ki = 226.0 nM 6.65
CHEMBL195849 Ki = 264.0 nM 6.58
CHEMBL193867 Ki = 325.0 nM 6.49
CHEMBL195047 Ki = 414.0 nM 6.38
CHEMBL193595 Ki = 430.0 nM 6.37
CHEMBL425567 Ki = 1175.0 nM 5.93
CHEMBL2112362 Ki = 1245.0 nM 5.91
CHEMBL2112360 Ki = 1330.0 nM 5.88