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Assay Detail

CHEMBL671652

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

Binding
Ability to displace [3H]spiperone from cloned human dopamine D2 receptor stably expressed in CHO cells
11
Total Activities
11
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 sar of 2- and 3-substituted 7-azaindoles as potential dopamine D4 ligands.
Curtis NR, Kulagowski JJ, Leeson PD, Ridgill MP, Emms F, Freedman SB, Patel S, Patel S.
Bioorg Med Chem Lett (1999) 9 : 585 -588
PubMed 10098669 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 6.34 7.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2112912 1 7.68
CHEMBL156732 1 6.70
CHEMBL2112913 1 6.55
CHEMBL156896 1 6.22
CHEMBL154286 1 6.19
CHEMBL347155 1 6.10
CHEMBL347291 1 6.05
CHEMBL267014 L-745870 1 6.02
CHEMBL155207 1 5.96
CHEMBL154482 1 5.89
CHEMBL28607 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2112912 Ki = 21.0 nM 7.68
CHEMBL156732 Ki = 200.0 nM 6.70
CHEMBL2112913 Ki = 280.0 nM 6.55
CHEMBL156896 Ki = 600.0 nM 6.22
CHEMBL154286 Ki = 640.0 nM 6.19
CHEMBL347155 Ki = 800.0 nM 6.10
CHEMBL347291 Ki = 900.0 nM 6.05
CHEMBL267014 L-745870 Ki = 960.0 nM 6.02
CHEMBL155207 Ki = 1100.0 nM 5.96
CHEMBL154482 Ki = 1300.0 nM 5.89
CHEMBL28607 Ki > 1500.0 nM -