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Assay Detail

CHEMBL675845

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

Binding
Potency of inhibiting 10 pM [125I]-RTI-55 binding to dopamine receptor in rat striatal membranes
13
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Subcellular Membrane
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Dopamine receptor (CHEMBL2093868)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Synthesis of methylphenidate analogues and their binding affinities at dopamine and serotonin transport sites.
Davies HM, Hopper DW, Hansen T, Liu Q, Childers SR.
Bioorg Med Chem Lett (2004) 14 : 1799 -1802
PubMed 15026075 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.65 8.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54134 1 8.57
CHEMBL300620 2 7.96
CHEMBL52154 1 7.47
CHEMBL50159 1 7.04
CHEMBL53342 1 6.94
CHEMBL904 DEXMETHYLPHENIDATE HYDROCHLORIDE 4.0 1 6.79
CHEMBL298583 1 5.99
CHEMBL51371 1 5.68
CHEMBL301775 1 5.56
CHEMBL52213 1 5.19
CHEMBL51101 1 5.13
CHEMBL50570 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54134 IC50 = 2.67 nM 8.57
CHEMBL300620 IC50 = 11.1 nM 7.96
CHEMBL300620 IC50 = 33.9 nM 7.47
CHEMBL52154 IC50 = 33.8 nM 7.47
CHEMBL50159 IC50 = 91.2 nM 7.04
CHEMBL53342 IC50 = 114.0 nM 6.94
CHEMBL904 DEXMETHYLPHENIDATE HYDROCHLORIDE IC50 = 164.0 nM 6.79
CHEMBL298583 IC50 = 1020.0 nM 5.99
CHEMBL51371 IC50 = 2080.0 nM 5.68
CHEMBL301775 IC50 = 2750.0 nM 5.56
CHEMBL52213 IC50 = 6470.0 nM 5.19
CHEMBL51101 IC50 = 7430.0 nM 5.13
CHEMBL50570 IC50 > 1000.0 nM -