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

CHEMBL829007

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

Functional
Effective concentration from [3H]thymidine uptake assay in CHO10001 cells expressing human Dopamine receptor D4.2
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO10001
Confidence 9 — Direct single protein target
Curated By Expert

Target

D(4) dopamine receptor (CHEMBL219)
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 8.06 9.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
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 9.26
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 8.92
CHEMBL194555 Fe complex 1 8.12
CHEMBL240773 QUINPIROLE 2.0 1 7.72
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 7.66
CHEMBL370297 Ruthenium complex 1 7.46
CHEMBL540612 1 7.31

Activity Data

Compound Name Type Rel. Value Units pChEMBL
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 = 0.55 nM 9.26
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 = 1.2 nM 8.92
CHEMBL194555 Fe complex EC50 = 7.6 nM 8.12
CHEMBL240773 QUINPIROLE EC50 = 19.0 nM 7.72
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 = 22.0 nM 7.66
CHEMBL370297 Ruthenium complex EC50 = 35.0 nM 7.46
CHEMBL540612 EC50 = 49.0 nM 7.31