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Assay Detail

CHEMBL829291

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

Functional
Effective concentration in [3H]thymidine uptake assay by CHO dhfr- mutant cells expressing human D3 receptor
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Expert

Target

D(3) dopamine receptor (CHEMBL234)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Fancy bioisosteres: metallocene-derived G-protein-coupled receptor ligands with subnanomolar binding affinity and novel selectivity profiles.
Schlotter K, Boeckler F, Hübner H, Gmeiner P.
J Med Chem (2005) 48 : 3696 -3699
PubMed 15916420 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 8.43 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL240773 QUINPIROLE 2.0 1 8.85
CHEMBL364516 N-{4-[4-(2-methoxyphenyl)piperazin-1-yl]butyl}-1-ferra-1,1'-spirobi[pentacyclo[2.2.0.0^{1,3}.0^{1,5}.0^{2,6}]hexane]-2,2',4,4'-tetraene-6-carboxamide 1 8.70
CHEMBL540612 1 8.57
CHEMBL194555 Fe complex 1 8.46
CHEMBL191962 N-{4-[4-(2-methoxyphenyl)piperazin-1-yl]butyl}-1-ruthena-1,1'-spirobi[pentacyclo[2.2.0.0^{1,3}.0^{1,5}.0^{2,6}]hexane]-2,2',4,4'-tetraene-6-carboxamide 1 8.41
CHEMBL370297 Ruthenium complex 1 8.04
CHEMBL195083 N-{4-[4-(3-chloro-2-methoxyphenyl)piperazin-1-yl]butyl}-1-ferra-1,1'-spirobi[pentacyclo[2.2.0.0^{1,3}.0^{1,5}.0^{2,6}]hexane]-2,2',4,4'-tetraene-6-carboxamide 1 8.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL240773 QUINPIROLE EC50 = 1.4 nM 8.85
CHEMBL364516 N-{4-[4-(2-methoxyphenyl)piperazin-1-yl]butyl}-1-ferra-1,1'-spirobi[pentacyclo[2.2.0.0^{1,3}.0^{1,5}.0^{2,6}]hexane]-2,2',4,4'-tetraene-6-carboxamide EC50 = 2.0 nM 8.70
CHEMBL540612 EC50 = 2.7 nM 8.57
CHEMBL194555 Fe complex EC50 = 3.5 nM 8.46
CHEMBL191962 N-{4-[4-(2-methoxyphenyl)piperazin-1-yl]butyl}-1-ruthena-1,1'-spirobi[pentacyclo[2.2.0.0^{1,3}.0^{1,5}.0^{2,6}]hexane]-2,2',4,4'-tetraene-6-carboxamide EC50 = 3.9 nM 8.41
CHEMBL370297 Ruthenium complex EC50 = 9.1 nM 8.04
CHEMBL195083 N-{4-[4-(3-chloro-2-methoxyphenyl)piperazin-1-yl]butyl}-1-ferra-1,1'-spirobi[pentacyclo[2.2.0.0^{1,3}.0^{1,5}.0^{2,6}]hexane]-2,2',4,4'-tetraene-6-carboxamide EC50 = 9.8 nM 8.01