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Assay Detail

CHEMBL2327306

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

Binding
Inhibition of human recombinant NET expressed in HEK cells
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sodium-dependent noradrenaline transporter (CHEMBL222)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Azepines and piperidines with dual norepinephrine dopamine uptake inhibition and antidepressant activity.
Brown DG, Bernstein PR, Wu Y, Urbanek RA, Becker CW, Throner SR, Dembofsky BT, Steelman GB, Lazor LA, Scott CW, Wood MW, Wesolowski SS, Nugiel DA, Koch S, Yu J, Pivonka DE, Li S, Thompson C, Zacco A, Elmore CS, Schroeder P, Liu J, Hurley CA, Ward S, Hunt HJ, Williams K, McLaughlin J, Hoesch V, Sydserff S, Maier D, Aharony D.
ACS Med Chem Lett (2013) 4 : 46 -51
PubMed 24900562 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 28 7.33 8.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2321991 1 8.48
CHEMBL2321993 1 8.40
CHEMBL51697 1 8.40
CHEMBL273575 NOMIFENSINE 4.0 1 8.30
CHEMBL2326695 1 8.29
CHEMBL2326693 1 7.92
CHEMBL2321996 1 7.92
CHEMBL2326694 1 7.82
CHEMBL2321999 1 7.77
CHEMBL2322000 1 7.62
CHEMBL2322001 1 7.60
CHEMBL2326690 1 7.34
CHEMBL2321990 1 7.31
CHEMBL2321997 1 7.27
CHEMBL2321995 1 7.24
CHEMBL2321998 1 7.18
CHEMBL2326691 1 7.13
CHEMBL2322002 1 7.08
CHEMBL2326689 1 6.92
CHEMBL2326684 1 6.89
CHEMBL2326686 1 6.89
CHEMBL2326692 1 6.89
CHEMBL2326685 1 6.77
CHEMBL2326687 1 6.60
CHEMBL2321992 1 6.60
CHEMBL2326688 1 6.37
CHEMBL2321994 1 6.37
CHEMBL400964 1 5.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2321991 Ki = 3.3 nM 8.48
CHEMBL2321993 Ki = 4.0 nM 8.40
CHEMBL51697 Ki = 4.0 nM 8.40
CHEMBL273575 NOMIFENSINE Ki = 5.0 nM 8.30
CHEMBL2326695 Ki = 5.1 nM 8.29
CHEMBL2326693 Ki = 12.0 nM 7.92
CHEMBL2321996 Ki = 12.0 nM 7.92
CHEMBL2326694 Ki = 15.0 nM 7.82
CHEMBL2321999 Ki = 17.0 nM 7.77
CHEMBL2322000 Ki = 24.0 nM 7.62
CHEMBL2322001 Ki = 25.0 nM 7.60
CHEMBL2326690 Ki = 46.0 nM 7.34
CHEMBL2321990 Ki = 49.0 nM 7.31
CHEMBL2321997 Ki = 54.0 nM 7.27
CHEMBL2321995 Ki = 57.0 nM 7.24
CHEMBL2321998 Ki = 66.0 nM 7.18
CHEMBL2326691 Ki = 74.0 nM 7.13
CHEMBL2322002 Ki = 83.0 nM 7.08
CHEMBL2326689 Ki = 120.0 nM 6.92
CHEMBL2326684 Ki = 130.0 nM 6.89
CHEMBL2326686 Ki = 130.0 nM 6.89
CHEMBL2326692 Ki = 130.0 nM 6.89
CHEMBL2326685 Ki = 170.0 nM 6.77
CHEMBL2326687 Ki = 250.0 nM 6.60
CHEMBL2321992 Ki = 250.0 nM 6.60
CHEMBL2326688 Ki = 430.0 nM 6.37
CHEMBL2321994 Ki = 430.0 nM 6.37
CHEMBL400964 Ki = 1200.0 nM 5.92