Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL674495

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

Binding
Ability to displace [3H]spiperone [0.5 nM (Kd=0.1-0.45 nM)] from human recombinant dopamine receptor D4 expressed in CHO cells
30
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Stereocontrolled dopamine receptor binding and subtype selectivity of clebopride analogues synthesized from aspartic acid.
Einsiedel J, Weber K, Thomas C, Lehmann T, Hübner H, Gmeiner P.
Bioorg Med Chem Lett (2003) 13 : 3293 -3296
PubMed 12951112 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 30 7.77 9.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL326454 2 9.64
CHEMBL111749 2 9.11
CHEMBL325772 2 8.92
CHEMBL109912 2 8.80
CHEMBL112833 2 8.60
CHEMBL321492 2 8.57
CHEMBL325109 CLEBOPRIDE 2.0 1 8.49
CHEMBL298875 2 8.30
CHEMBL322802 2 8.13
CHEMBL112395 1 8.08
CHEMBL430522 2 7.77
CHEMBL447476 2 7.60
CHEMBL325818 2 7.11
CHEMBL112831 2 6.70
CHEMBL113471 2 6.30
CHEMBL109472 2 6.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL326454 Ki = 0.23 nM 9.64
CHEMBL111749 Ki = 0.77 nM 9.11
CHEMBL326454 Ki = 0.84 nM 9.08
CHEMBL325772 Ki = 1.2 nM 8.92
CHEMBL109912 Ki = 1.6 nM 8.80
CHEMBL112833 Ki = 2.5 nM 8.60
CHEMBL321492 Ki = 2.7 nM 8.57
CHEMBL325109 CLEBOPRIDE Ki = 3.2 nM 8.49
CHEMBL325772 Ki = 3.3 nM 8.48
CHEMBL111749 Ki = 4.3 nM 8.37
CHEMBL109912 Ki = 4.7 nM 8.33
CHEMBL298875 Ki = 5.0 nM 8.30
CHEMBL112833 Ki = 7.0 nM 8.15
CHEMBL322802 Ki = 7.4 nM 8.13
CHEMBL112395 Ki = 8.3 nM 8.08
CHEMBL430522 Ki = 17.0 nM 7.77
CHEMBL298875 Ki = 21.0 nM 7.68
CHEMBL447476 Ki = 25.0 nM 7.60
CHEMBL321492 Ki = 27.0 nM 7.57
CHEMBL322802 Ki = 35.0 nM 7.46
CHEMBL430522 Ki = 59.0 nM 7.23
CHEMBL447476 Ki = 64.0 nM 7.19
CHEMBL325818 Ki = 78.0 nM 7.11
CHEMBL325818 Ki = 130.0 nM 6.89
CHEMBL112831 Ki = 200.0 nM 6.70
CHEMBL109472 Ki = 500.0 nM 6.30
CHEMBL113471 Ki = 500.0 nM 6.30
CHEMBL112831 Ki = 530.0 nM 6.28
CHEMBL113471 Ki = 610.0 nM 6.21
CHEMBL109472 Ki = 1500.0 nM 5.82