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Assay Detail

CHEMBL961043

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

Binding
Inhibition of human cloned dopamine D4 receptor by competitive binding experiment
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Synthesis and in vitro affinities of various MDL 100907 derivatives as potential 18F-radioligands for 5-HT2A receptor imaging with PET.
Herth MM, Kramer V, Piel M, Palner M, Riss PJ, Knudsen GM, Rösch F.
Bioorg Med Chem (2009) 17 : 2989 -3002
PubMed 19329329 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 6.20 6.76

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL516088 1 6.76
CHEMBL515472 1 6.36
CHEMBL402143 1 6.26
CHEMBL490632 1 6.04
CHEMBL476839 1 5.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL516088 Ki = 174.0 nM 6.76
CHEMBL515472 Ki = 442.0 nM 6.36
CHEMBL402143 Ki = 544.0 nM 6.26
CHEMBL490632 Ki = 923.0 nM 6.04
CHEMBL476839 Ki = 2708.0 nM 5.57