Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL1041760

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

Binding
Displacement of [125I]RTI55 from cloned human NET expressed in HEK293 cells
38
Total Activities
38
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 Intermediate

Target

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

Publication

Synthesis and biological evaluation of bupropion analogues as potential pharmacotherapies for cocaine addiction.
Carroll FI, Blough BE, Abraham P, Mills AC, Holleman JA, Wolckenhauer SA, Decker AM, Landavazo A, McElroy KT, Navarro HA, Gatch MB, Forster MJ.
J Med Chem (2009) 52 : 6768 -6781
PubMed 19821577 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 38 5.50 6.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL566050 1 6.28
CHEMBL370805 COCAINE 4.0 1 6.08
CHEMBL569465 1 5.93
CHEMBL566418 1 5.75
CHEMBL566208 1 5.65
CHEMBL565594 1 5.64
CHEMBL565593 1 5.59
CHEMBL566830 1 5.51
CHEMBL576622 1 5.50
CHEMBL566886 1 5.50
CHEMBL567479 1 5.42
CHEMBL569700 1 5.40
CHEMBL565382 1 5.37
CHEMBL578815 1 5.35
CHEMBL565845 1 5.34
CHEMBL566420 1 5.32
CHEMBL565844 1 5.29
CHEMBL568140 1 5.27
CHEMBL569699 1 5.24
CHEMBL566618 1 5.24
CHEMBL566207 1 5.17
CHEMBL894 BUPROPION 4.0 1 5.16
CHEMBL565396 1 -
CHEMBL566193 1 -
CHEMBL157455 1 -
CHEMBL576063 1 -
CHEMBL566832 1 -
CHEMBL566000 1 -
CHEMBL566001 1 -
CHEMBL578610 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL566050 Ki = 520.0 nM 6.28
CHEMBL370805 COCAINE Ki = 830.0 nM 6.08
CHEMBL569465 Ki = 1171.0 nM 5.93
CHEMBL566418 Ki = 1800.0 nM 5.75
CHEMBL566208 Ki = 2240.0 nM 5.65
CHEMBL565594 Ki = 2300.0 nM 5.64
CHEMBL565593 Ki = 2580.0 nM 5.59
CHEMBL566830 Ki = 3090.0 nM 5.51
CHEMBL576622 Ki = 3190.0 nM 5.50
CHEMBL566886 Ki = 3195.0 nM 5.50
CHEMBL567479 Ki = 3800.0 nM 5.42
CHEMBL569700 Ki = 4000.0 nM 5.40
CHEMBL565382 Ki = 4300.0 nM 5.37
CHEMBL578815 Ki = 4476.0 nM 5.35
CHEMBL565845 Ki = 4600.0 nM 5.34
CHEMBL566420 Ki = 4760.0 nM 5.32
CHEMBL565844 Ki = 5100.0 nM 5.29
CHEMBL568140 Ki = 5400.0 nM 5.27
CHEMBL566618 Ki = 5700.0 nM 5.24
CHEMBL569699 Ki = 5700.0 nM 5.24
CHEMBL566207 Ki = 6840.0 nM 5.17
CHEMBL894 BUPROPION Ki = 6970.0 nM 5.16
CHEMBL567482 Ki > 10000.0 nM -
CHEMBL567481 Ki > 10000.0 nM -
CHEMBL565386 Ki > 10000.0 nM -
CHEMBL578612 Ki > 10000.0 nM -
CHEMBL565397 Ki > 10000.0 nM -
CHEMBL567480 Ki > 10000.0 nM -
CHEMBL578611 Ki > 10000.0 nM -
CHEMBL577501 Ki > 10000.0 nM -
CHEMBL578610 Ki > 10000.0 nM -
CHEMBL566001 Ki > 10000.0 nM -
CHEMBL566000 Ki > 10000.0 nM -
CHEMBL566832 Ki > 10000.0 nM -
CHEMBL576063 Ki > 10000.0 nM -
CHEMBL157455 Ki > 10000.0 nM -
CHEMBL566193 Ki > 10000.0 nM -
CHEMBL565396 Ki > 7140.0 nM -