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Assay Detail

CHEMBL672383

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

Binding
Displacement of [3H]spiperone from human Dopamine receptor D2L expressed in CHO cells
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 Expert

Target

D(2) dopamine receptor (CHEMBL217)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Cyanoindole derivatives as highly selective dopamine D(4) receptor partial agonists: solid-phase synthesis, binding assays, and functional experiments.
Hübner H, Kraxner J, Gmeiner P.
J Med Chem (2000) 43 : 4563 -4569
PubMed 11087581 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 5.52 7.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL42 CLOZAPINE 4.0 1 7.39
CHEMBL140258 1 6.30
CHEMBL344270 1 6.10
CHEMBL143355 1 5.85
CHEMBL344602 1 5.70
CHEMBL141035 1 5.64
CHEMBL140165 1 5.62
CHEMBL140099 1 5.51
CHEMBL342001 1 5.37
CHEMBL343880 1 5.25
CHEMBL140594 1 5.10
CHEMBL143761 1 4.55
CHEMBL142217 1 4.47
CHEMBL140006 1 4.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL42 CLOZAPINE Ki = 41.0 nM 7.39
CHEMBL140258 Ki = 500.0 nM 6.30
CHEMBL344270 Ki = 790.0 nM 6.10
CHEMBL143355 Ki = 1400.0 nM 5.85
CHEMBL344602 Ki = 2000.0 nM 5.70
CHEMBL141035 Ki = 2300.0 nM 5.64
CHEMBL140165 Ki = 2400.0 nM 5.62
CHEMBL140099 Ki = 3100.0 nM 5.51
CHEMBL342001 Ki = 4300.0 nM 5.37
CHEMBL343880 Ki = 5600.0 nM 5.25
CHEMBL140594 Ki = 7900.0 nM 5.10
CHEMBL143761 Ki = 28000.0 nM 4.55
CHEMBL142217 Ki = 34000.0 nM 4.47
CHEMBL140006 Ki = 43000.0 nM 4.37