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Assay Detail

CHEMBL2343889

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Binding
Inhibition of human recombinant SERT expressed in HEK293 cells assessed as inhibition of [3H]5HT reuptake
ChEMBL ↗
51
Total Activities
51
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 serotonin transporter (CHEMBL228) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A novel class of 3-(phenoxy-phenyl-methyl)-pyrrolidines as potent and balanced norepinephrine and serotonin reuptake inhibitors: synthesis and structure-activity relationships.
Van Orden LJ, Van Dyke PM, Saito DR, Church TJ, Chang R, Smith JA, Martin WJ, Jaw-Tsai S, Stangeland EL.
Bioorg Med Chem Lett (2013) 23 : 1456 -1461
PubMed 23347683 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 51 8.04 9.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1175 DULOXETINE 4.0 1 9.50
CHEMBL2338047 — — 1 9.30
CHEMBL2337599 — — 1 9.20
CHEMBL2338037 — — 1 9.20
CHEMBL2337608 — — 1 9.10
CHEMBL2337603 — — 1 9.10
CHEMBL2338039 — — 1 9.00
CHEMBL2338049 — — 1 9.00
CHEMBL2337597 — — 1 8.90
CHEMBL2338036 — — 1 8.90
CHEMBL2338041 — — 1 8.80
CHEMBL2338038 — — 1 8.80
CHEMBL2337600 — — 1 8.70
CHEMBL2337595 — — 1 8.60
CHEMBL2337604 — — 1 8.50
CHEMBL2338042 — — 1 8.40
CHEMBL2338046 — — 1 8.40
CHEMBL2337593 — — 1 8.40
CHEMBL2338033 — — 1 8.40
CHEMBL2338043 — — 1 8.40
CHEMBL2338050 — — 1 8.30
CHEMBL2338053 — — 1 8.30
CHEMBL2337607 — — 1 8.20
CHEMBL2338054 — — 1 8.20
CHEMBL2338051 — — 1 8.20
CHEMBL2337596 — — 1 8.10
CHEMBL2338031 — — 1 8.10
CHEMBL2338045 — — 1 8.10
CHEMBL2337602 — — 1 8.00
CHEMBL2337605 — — 1 8.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1175 DULOXETINE IC50 = 0.3162 nM 9.50
CHEMBL2338047 — IC50 = 0.5012 nM 9.30
CHEMBL2337599 — IC50 = 0.631 nM 9.20
CHEMBL2338037 — IC50 = 0.631 nM 9.20
CHEMBL2337608 — IC50 = 0.7943 nM 9.10
CHEMBL2337603 — IC50 = 0.7943 nM 9.10
CHEMBL2338039 — IC50 = 1.0 nM 9.00
CHEMBL2338049 — IC50 = 1.0 nM 9.00
CHEMBL2338036 — IC50 = 1.259 nM 8.90
CHEMBL2337597 — IC50 = 1.259 nM 8.90
CHEMBL2338041 — IC50 = 1.585 nM 8.80
CHEMBL2338038 — IC50 = 1.585 nM 8.80
CHEMBL2337600 — IC50 = 1.995 nM 8.70
CHEMBL2337595 — IC50 = 2.512 nM 8.60
CHEMBL2337604 — IC50 = 3.162 nM 8.50
CHEMBL2338042 — IC50 = 3.981 nM 8.40
CHEMBL2338043 — IC50 = 3.981 nM 8.40
CHEMBL2338033 — IC50 = 3.981 nM 8.40
CHEMBL2337593 — IC50 = 3.981 nM 8.40
CHEMBL2338046 — IC50 = 3.981 nM 8.40
CHEMBL2338050 — IC50 = 5.012 nM 8.30
CHEMBL2338053 — IC50 = 5.012 nM 8.30
CHEMBL2337607 — IC50 = 6.31 nM 8.20
CHEMBL2338054 — IC50 = 6.31 nM 8.20
CHEMBL2338051 — IC50 = 6.31 nM 8.20
CHEMBL2337596 — IC50 = 7.943 nM 8.10
CHEMBL2338045 — IC50 = 7.943 nM 8.10
CHEMBL2338031 — IC50 = 7.943 nM 8.10
CHEMBL2337602 — IC50 = 10.0 nM 8.00
CHEMBL2337605 — IC50 = 10.0 nM 8.00
CHEMBL2337591 — IC50 = 12.59 nM 7.90
CHEMBL2338034 — IC50 = 12.59 nM 7.90
CHEMBL2338048 — IC50 = 15.85 nM 7.80
CHEMBL2338035 — IC50 = 15.85 nM 7.80
CHEMBL2337598 — IC50 = 19.95 nM 7.70
CHEMBL2338040 — IC50 = 25.12 nM 7.60
CHEMBL2337594 — IC50 = 31.62 nM 7.50
CHEMBL2338055 — IC50 = 31.62 nM 7.50
CHEMBL2337606 — IC50 = 39.81 nM 7.40
CHEMBL259209 MILNACIPRAN IC50 = 50.12 nM 7.30
CHEMBL2337601 — IC50 = 63.1 nM 7.20
CHEMBL2338044 — IC50 = 63.1 nM 7.20
CHEMBL2337590 — IC50 = 63.1 nM 7.20
CHEMBL2338052 — IC50 = 79.43 nM 7.10
CHEMBL2337587 — IC50 = 100.0 nM 7.00
CHEMBL2337589 — IC50 = 125.89 nM 6.90
CHEMBL2337592 — IC50 = 125.89 nM 6.90
CHEMBL2337586 — IC50 = 158.49 nM 6.80
CHEMBL2337588 — IC50 = 158.49 nM 6.80
CHEMBL2338032 — IC50 = 158.49 nM 6.80