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Assay Detail

CHEMBL5235422

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

Binding
Displacement of [3H]-spiperone from human D4 receptor expressed in CHO cells assessed as inhibition constant
14
Total Activities
14
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 Autocuration

Target

D(4) dopamine receptor (CHEMBL219)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Recent findings leading to the discovery of selective dopamine D<sub>4</sub> receptor ligands for the treatment of widespread diseases.
Giorgioni G, Del Bello F, Pavletić P, Quaglia W, Botticelli L, Cifani C, Micioni Di Bonaventura E, Micioni Di Bonaventura MV, Piergentili A.
Eur J Med Chem (2021) 212 : 113141 -113141
PubMed 33422983 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 8.86 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2207643 1 9.40
CHEMBL5285358 1 9.30
CHEMBL140099 1 9.28
CHEMBL5272162 1 9.18
CHEMBL5278853 1 9.12
CHEMBL143761 1 9.00
CHEMBL160626 1 8.82
CHEMBL5280364 1 8.82
CHEMBL104035 1 8.70
CHEMBL310843 1 8.66
CHEMBL108122 1 8.55
CHEMBL7927 FAUC 113 1 8.51
CHEMBL346389 1 8.37
CHEMBL1616116 1 8.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2207643 Ki = 0.4 nM 9.40
CHEMBL5285358 Ki = 0.5 nM 9.30
CHEMBL140099 Ki = 0.52 nM 9.28
CHEMBL5272162 Ki = 0.66 nM 9.18
CHEMBL5278853 Ki = 0.76 nM 9.12
CHEMBL143761 Ki = 1.0 nM 9.00
CHEMBL160626 Ki = 1.5 nM 8.82
CHEMBL5280364 Ki = 1.5 nM 8.82
CHEMBL104035 Ki = 2.0 nM 8.70
CHEMBL310843 Ki = 2.2 nM 8.66
CHEMBL108122 Ki = 2.8 nM 8.55
CHEMBL7927 FAUC 113 Ki = 3.1 nM 8.51
CHEMBL346389 Ki = 4.3 nM 8.37
CHEMBL1616116 Ki = 5.2 nM 8.28