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Assay Detail

CHEMBL930495

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Binding
Inhibition of human SERT
ChEMBL ↗
47
Total Activities
46
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Sodium-dependent serotonin transporter (CHEMBL228) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of 1S,2R-milnacipran analogs as potent norepinephrine and serotonin transporter inhibitors.
Tamiya J, Dyck B, Zhang M, Phan K, Fleck BA, Aparicio A, Jovic F, Tran JA, Vickers T, Grey J, Foster AC, Chen C.
Bioorg Med Chem Lett (2008) 18 : 3328 -3332
PubMed 18445525 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 47 6.68 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL260440 — — 1 7.89
CHEMBL410015 — — 1 7.85
CHEMBL402441 — — 1 7.60
CHEMBL264430 — — 1 7.58
CHEMBL409715 — — 1 7.55
CHEMBL256557 — — 1 7.50
CHEMBL404729 — — 1 7.41
CHEMBL408384 — — 1 7.31
CHEMBL258451 — — 1 7.27
CHEMBL259694 — — 1 7.24
CHEMBL427904 — — 1 7.19
CHEMBL260863 — — 1 7.19
CHEMBL411033 — — 1 7.11
CHEMBL257335 — — 1 7.00
CHEMBL405613 — — 1 6.95
CHEMBL260131 — — 1 6.90
CHEMBL408940 — — 1 6.89
CHEMBL264678 — — 1 6.85
CHEMBL411677 — — 1 6.84
CHEMBL406789 — — 1 6.82
CHEMBL257336 — — 1 6.80
CHEMBL641 ATOMOXETINE 4.0 1 6.72
CHEMBL404730 — — 1 6.68
CHEMBL410054 — — 1 6.68
CHEMBL404013 — — 1 6.57
CHEMBL260439 — — 1 6.55
CHEMBL258450 — — 1 6.55
CHEMBL411655 — — 1 6.50
CHEMBL99946 LEVOMILNACIPRAN 4.0 1 6.50
CHEMBL404145 — — 1 6.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL260440 — IC50 = 13.0 nM 7.89
CHEMBL410015 — IC50 = 14.0 nM 7.85
CHEMBL402441 — IC50 = 25.0 nM 7.60
CHEMBL264430 — IC50 = 26.0 nM 7.58
CHEMBL409715 — IC50 = 28.0 nM 7.55
CHEMBL256557 — IC50 = 32.0 nM 7.50
CHEMBL404729 — IC50 = 39.0 nM 7.41
CHEMBL408384 — IC50 = 49.0 nM 7.31
CHEMBL258451 — IC50 = 54.0 nM 7.27
CHEMBL259694 — IC50 = 58.0 nM 7.24
CHEMBL427904 — IC50 = 65.0 nM 7.19
CHEMBL260863 — IC50 = 64.0 nM 7.19
CHEMBL411033 — IC50 = 77.0 nM 7.11
CHEMBL257335 — IC50 = 100.0 nM 7.00
CHEMBL405613 — IC50 = 112.0 nM 6.95
CHEMBL260131 — IC50 = 125.0 nM 6.90
CHEMBL408940 — IC50 = 130.0 nM 6.89
CHEMBL264678 — IC50 = 140.0 nM 6.85
CHEMBL411677 — IC50 = 145.0 nM 6.84
CHEMBL406789 — IC50 = 150.0 nM 6.82
CHEMBL257336 — IC50 = 160.0 nM 6.80
CHEMBL641 ATOMOXETINE IC50 = 190.0 nM 6.72
CHEMBL410054 — IC50 = 210.0 nM 6.68
CHEMBL404730 — IC50 = 210.0 nM 6.68
CHEMBL404013 — IC50 = 270.0 nM 6.57
CHEMBL260439 — IC50 = 280.0 nM 6.55
CHEMBL258450 — IC50 = 280.0 nM 6.55
CHEMBL411655 — IC50 = 320.0 nM 6.50
CHEMBL99946 LEVOMILNACIPRAN IC50 = 320.0 nM 6.50
CHEMBL404145 — IC50 = 370.0 nM 6.43
CHEMBL259209 MILNACIPRAN IC50 = 420.0 nM 6.38
CHEMBL258180 — IC50 = 430.0 nM 6.37
CHEMBL410055 — IC50 = 460.0 nM 6.34
CHEMBL405728 — IC50 = 480.0 nM 6.32
CHEMBL260988 — IC50 = 480.0 nM 6.32
CHEMBL408016 — IC50 = 540.0 nM 6.27
CHEMBL257550 — IC50 = 560.0 nM 6.25
CHEMBL255303 — IC50 = 1100.0 nM 5.96
CHEMBL403469 — IC50 = 1700.0 nM 5.77
CHEMBL403949 — IC50 = 2100.0 nM 5.68
CHEMBL257549 — IC50 = 3400.0 nM 5.47
CHEMBL259209 MILNACIPRAN IC50 = 3500.0 nM 5.46
CHEMBL257551 — IC50 = 6400.0 nM 5.19
CHEMBL405462 — IC50 = 6900.0 nM 5.16
CHEMBL410062 — IC50 > 10000.0 nM -
CHEMBL260335 — IC50 > 10000.0 nM -
CHEMBL260336 — IC50 > 10000.0 nM -