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Assay Detail

CHEMBL871243

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

Binding
Displacement of [3H]spiperone from human cloned dopamine D2(short) receptor expressed in CHO cells
16
Total Activities
16
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(2) dopamine receptor (CHEMBL217)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological investigations of dopaminergic partial agonists preferentially recognizing the D4 receptor subtype.
Löber S, Hübner H, Gmeiner P.
Bioorg Med Chem Lett (2006) 16 : 2955 -2959
PubMed 16563764 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 6.75 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL379602 1 8.10
CHEMBL378455 1 7.55
CHEMBL210404 1 7.51
CHEMBL210717 1 7.43
CHEMBL208018 1 7.37
CHEMBL210232 1 7.19
CHEMBL210405 1 7.12
CHEMBL379177 1 6.96
CHEMBL60815 1 6.77
CHEMBL425057 1 6.72
CHEMBL377200 1 6.60
CHEMBL437490 1 6.40
CHEMBL211026 1 6.07
CHEMBL210955 1 5.72
CHEMBL210318 1 5.62
CHEMBL209832 1 4.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL379602 Ki = 8.0 nM 8.10
CHEMBL378455 Ki = 28.0 nM 7.55
CHEMBL210404 Ki = 31.0 nM 7.51
CHEMBL210717 Ki = 37.0 nM 7.43
CHEMBL208018 Ki = 43.0 nM 7.37
CHEMBL210232 Ki = 65.0 nM 7.19
CHEMBL210405 Ki = 75.0 nM 7.12
CHEMBL379177 Ki = 110.0 nM 6.96
CHEMBL60815 Ki = 170.0 nM 6.77
CHEMBL425057 Ki = 190.0 nM 6.72
CHEMBL377200 Ki = 250.0 nM 6.60
CHEMBL437490 Ki = 400.0 nM 6.40
CHEMBL211026 Ki = 860.0 nM 6.07
CHEMBL210955 Ki = 1900.0 nM 5.72
CHEMBL210318 Ki = 2400.0 nM 5.62
CHEMBL209832 Ki = 14000.0 nM 4.85