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Assay Detail

CHEMBL2215841

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

Binding
Inhibition of SERT-mediated [3H]5HT uptake in rat synaptosomes by scintillation counting
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sodium-dependent serotonin transporter (CHEMBL313)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Discovery of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine (Lu AA21004): a novel multimodal compound for the treatment of major depressive disorder.
Bang-Andersen B, Ruhland T, Jørgensen M, Smith G, Frederiksen K, Jensen KG, Zhong H, Nielsen SM, Hogg S, Mørk A, Stensbøl TB.
J Med Chem (2011) 54 : 3206 -3221
PubMed 21486038 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 38 7.51 8.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL549 CITALOPRAM 4.0 1 8.41
CHEMBL2204361 1 8.37
CHEMBL2204357 1 8.36
CHEMBL2205053 1 8.33
CHEMBL2204359 1 8.28
CHEMBL2204360 1 8.28
CHEMBL2205054 1 8.24
CHEMBL2205046 1 8.16
CHEMBL2204358 1 8.12
CHEMBL2205037 1 8.10
CHEMBL2205042 1 8.10
CHEMBL2205038 1 8.02
CHEMBL2204363 1 8.01
CHEMBL2204362 1 7.96
CHEMBL2205043 1 7.89
CHEMBL2205052 1 7.82
CHEMBL2204356 1 7.77
CHEMBL2205045 1 7.75
CHEMBL2205040 1 7.70
CHEMBL2204365 1 7.60
CHEMBL2204355 1 7.43
CHEMBL2204364 1 7.36
CHEMBL2205051 1 7.29
CHEMBL2205048 1 7.28
CHEMBL2205049 1 7.27
CHEMBL2205044 1 7.17
CHEMBL2205039 1 7.17
CHEMBL2205034 1 6.89
CHEMBL2205036 1 6.82
CHEMBL2205031 1 6.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL549 CITALOPRAM IC50 = 3.9 nM 8.41
CHEMBL2204361 IC50 = 4.3 nM 8.37
CHEMBL2204357 IC50 = 4.4 nM 8.36
CHEMBL2205053 IC50 = 4.7 nM 8.33
CHEMBL2204359 IC50 = 5.2 nM 8.28
CHEMBL2204360 IC50 = 5.3 nM 8.28
CHEMBL2205054 IC50 = 5.8 nM 8.24
CHEMBL2205046 IC50 = 6.9 nM 8.16
CHEMBL2204358 IC50 = 7.6 nM 8.12
CHEMBL2205037 IC50 = 7.9 nM 8.10
CHEMBL2205042 IC50 = 8.0 nM 8.10
CHEMBL2205038 IC50 = 9.5 nM 8.02
CHEMBL2204363 IC50 = 9.7 nM 8.01
CHEMBL2204362 IC50 = 11.0 nM 7.96
CHEMBL2205043 IC50 = 13.0 nM 7.89
CHEMBL2205052 IC50 = 15.0 nM 7.82
CHEMBL2204356 IC50 = 17.0 nM 7.77
CHEMBL2205045 IC50 = 18.0 nM 7.75
CHEMBL2205040 IC50 = 20.0 nM 7.70
CHEMBL2204365 IC50 = 25.0 nM 7.60
CHEMBL2204355 IC50 = 37.0 nM 7.43
CHEMBL2204364 IC50 = 44.0 nM 7.36
CHEMBL2205051 IC50 = 51.0 nM 7.29
CHEMBL2205048 IC50 = 53.0 nM 7.28
CHEMBL2205049 IC50 = 54.0 nM 7.27
CHEMBL2205044 IC50 = 67.0 nM 7.17
CHEMBL2205039 IC50 = 68.0 nM 7.17
CHEMBL2205034 IC50 = 130.0 nM 6.89
CHEMBL2205036 IC50 = 150.0 nM 6.82
CHEMBL2205031 IC50 = 200.0 nM 6.70
CHEMBL2205035 IC50 = 250.0 nM 6.60
CHEMBL2205050 IC50 = 330.0 nM 6.48
CHEMBL2205041 IC50 = 390.0 nM 6.41
CHEMBL2205032 IC50 = 540.0 nM 6.27
CHEMBL2205033 IC50 = 680.0 nM 6.17
CHEMBL2205047 IC50 = 2100.0 nM 5.68
CHEMBL49 BUSPIRONE IC50 > 1000.0 nM -
CHEMBL46 ONDANSETRON IC50 > 2000.0 nM -