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Assay Detail

CHEMBL747998

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

Binding
Displacement of from norepinephrine transporter of frozen rat caudate membranes
11
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Expert

Target

Norepinephrine transporter (CHEMBL304)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and pharmacological evaluation of 3-(3,4-dichlorophenyl)-1-indanamine derivatives as nonselective ligands for biogenic amine transporters.
Yu H, Kim IJ, Folk JE, Tian X, Rothman RB, Baumann MH, Dersch CM, Flippen-Anderson JL, Parrish D, Jacobson AE, Rice KC.
J Med Chem (2004) 47 : 2624 -2634
PubMed 15115403 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 7.10 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL296602 INDATRALINE 2.0 1 8.22
CHEMBL543372 1 8.15
CHEMBL89142 1 8.05
CHEMBL300019 2 7.82
CHEMBL301514 1 7.62
CHEMBL89752 1 6.36
CHEMBL554565 1 6.09
CHEMBL316341 2 6.00
CHEMBL315697 1 5.88

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL296602 INDATRALINE Ki = 6.0 nM 8.22
CHEMBL543372 Ki = 7.0 nM 8.15
CHEMBL89142 Ki = 9.0 nM 8.05
CHEMBL300019 Ki = 15.0 nM 7.82
CHEMBL301514 Ki = 24.0 nM 7.62
CHEMBL300019 Ki = 170.0 nM 6.77
CHEMBL89752 Ki = 440.0 nM 6.36
CHEMBL554565 Ki = 820.0 nM 6.09
CHEMBL316341 Ki = 1010.0 nM 6.00
CHEMBL315697 Ki = 1330.0 nM 5.88
CHEMBL316341 Ki > 4700.0 nM -