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Assay Detail

CHEMBL2343887

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Binding
Displacement of [3H]WIN35428 from human recombinant DAT transfected in HEK293 cell membrane
ChEMBL ↗
51
Total Activities
51
Compounds Tested
2
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 dopamine transporter (CHEMBL238) ↗
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
Ki 48 6.93 8.50
pKi 3 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2337603 — — 1 8.50
CHEMBL2338049 — — 1 8.10
CHEMBL2338047 — — 1 8.10
CHEMBL2338048 — — 1 7.90
CHEMBL2337596 — — 1 7.80
CHEMBL2338034 — — 1 7.50
CHEMBL2337595 — — 1 7.50
CHEMBL2337602 — — 1 7.40
CHEMBL2338039 — — 1 7.40
CHEMBL2337604 — — 1 7.40
CHEMBL2337593 — — 1 7.30
CHEMBL2338050 — — 1 7.20
CHEMBL2338051 — — 1 7.20
CHEMBL2338032 — — 1 7.20
CHEMBL2337592 — — 1 7.20
CHEMBL2338053 — — 1 7.10
CHEMBL2338055 — — 1 7.00
CHEMBL2338033 — — 1 7.00
CHEMBL2338054 — — 1 7.00
CHEMBL2338035 — — 1 7.00
CHEMBL2338042 — — 1 7.00
CHEMBL2338043 — — 1 7.00
CHEMBL2338045 — — 1 7.00
CHEMBL2338052 — — 1 7.00
CHEMBL2337594 — — 1 6.90
CHEMBL2338037 — — 1 6.90
CHEMBL2337591 — — 1 6.90
CHEMBL2338044 — — 1 6.90
CHEMBL2337605 — — 1 6.90
CHEMBL2337598 — — 1 6.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2337603 — Ki = 3.162 nM 8.50
CHEMBL2338049 — Ki = 7.943 nM 8.10
CHEMBL2338047 — Ki = 7.943 nM 8.10
CHEMBL2338048 — Ki = 12.59 nM 7.90
CHEMBL2337596 — Ki = 15.85 nM 7.80
CHEMBL2338034 — Ki = 31.62 nM 7.50
CHEMBL2337595 — Ki = 31.62 nM 7.50
CHEMBL2337602 — Ki = 39.81 nM 7.40
CHEMBL2338039 — Ki = 39.81 nM 7.40
CHEMBL2337604 — Ki = 39.81 nM 7.40
CHEMBL2337593 — Ki = 50.12 nM 7.30
CHEMBL2338032 — Ki = 63.1 nM 7.20
CHEMBL2337592 — Ki = 63.1 nM 7.20
CHEMBL2338051 — Ki = 63.1 nM 7.20
CHEMBL2338050 — Ki = 63.1 nM 7.20
CHEMBL2338053 — Ki = 79.43 nM 7.10
CHEMBL2338055 — Ki = 100.0 nM 7.00
CHEMBL2338033 — Ki = 100.0 nM 7.00
CHEMBL2338054 — Ki = 100.0 nM 7.00
CHEMBL2338035 — Ki = 100.0 nM 7.00
CHEMBL2338042 — Ki = 100.0 nM 7.00
CHEMBL2338043 — Ki = 100.0 nM 7.00
CHEMBL2338045 — Ki = 100.0 nM 7.00
CHEMBL2338052 — Ki = 100.0 nM 7.00
CHEMBL2338037 — Ki = 125.89 nM 6.90
CHEMBL2337598 — Ki = 125.89 nM 6.90
CHEMBL2337605 — Ki = 125.89 nM 6.90
CHEMBL2337591 — Ki = 125.89 nM 6.90
CHEMBL2337594 — Ki = 125.89 nM 6.90
CHEMBL2338044 — Ki = 125.89 nM 6.90
CHEMBL2337597 — Ki = 158.49 nM 6.80
CHEMBL2337590 — Ki = 158.49 nM 6.80
CHEMBL2337608 — Ki = 158.49 nM 6.80
CHEMBL2338031 — Ki = 158.49 nM 6.80
CHEMBL2337589 — Ki = 251.19 nM 6.60
CHEMBL2338046 — Ki = 316.23 nM 6.50
CHEMBL2337607 — Ki = 316.23 nM 6.50
CHEMBL2337606 — Ki = 316.23 nM 6.50
CHEMBL1175 DULOXETINE Ki = 316.23 nM 6.50
CHEMBL2338041 — Ki = 398.11 nM 6.40
CHEMBL2338036 — Ki = 398.11 nM 6.40
CHEMBL2337587 — Ki = 501.19 nM 6.30
CHEMBL2338040 — Ki = 794.33 nM 6.10
CHEMBL2337588 — Ki = 1000.0 nM 6.00
CHEMBL2337586 — Ki = 1000.0 nM 6.00
CHEMBL2338038 — Ki = 2511.89 nM 5.60
CHEMBL180101 ESREBOXETINE Ki = 19952.62 nM 4.70
CHEMBL2337600 — pKi - — -
CHEMBL2337601 — pKi - — -
CHEMBL259209 MILNACIPRAN Ki > 31622.78 nM -