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Assay Detail

CHEMBL674428

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

Binding
Binding affinity against Dopamine transporter using [125]RTI-55
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Sodium-dependent dopamine transporter (CHEMBL338)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and biological evaluation of tropane-like 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine (GBR 12909) analogues.
Zhang Y, Joseph DB, Bowen WD, Flippen-Anderson JL, Dersch CM, Rothman RB, Jacobson AE, Rice KC.
J Med Chem (2001) 44 : 3937 -3945
PubMed 11689080 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 6.94 8.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL281594 VANOXERINE 3.0 1 8.43
CHEMBL26320 1 8.43
CHEMBL129193 1 7.72
CHEMBL3084919 1 7.72
CHEMBL3084920 1 7.55
CHEMBL3084918 1 7.52
CHEMBL126235 1 7.28
CHEMBL130643 1 6.89
CHEMBL1201203 BENZTROPINE 4.0 1 6.62
CHEMBL3084921 1 6.57
CHEMBL3084922 1 6.55
CHEMBL339614 1 6.30
CHEMBL415721 1 5.64
CHEMBL127053 1 5.47
CHEMBL126735 1 5.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL281594 VANOXERINE Ki = 3.7 nM 8.43
CHEMBL26320 Ki = 3.7 nM 8.43
CHEMBL129193 Ki = 19.0 nM 7.72
CHEMBL3084919 Ki = 19.0 nM 7.72
CHEMBL3084920 Ki = 28.0 nM 7.55
CHEMBL3084918 Ki = 30.0 nM 7.52
CHEMBL126235 Ki = 52.0 nM 7.28
CHEMBL130643 Ki = 130.0 nM 6.89
CHEMBL1201203 BENZTROPINE Ki = 237.0 nM 6.62
CHEMBL3084921 Ki = 270.0 nM 6.57
CHEMBL3084922 Ki = 280.0 nM 6.55
CHEMBL339614 Ki = 500.0 nM 6.30
CHEMBL415721 Ki = 2300.0 nM 5.64
CHEMBL127053 Ki = 3400.0 nM 5.47
CHEMBL126735 Ki = 3800.0 nM 5.42