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Assay Detail

CHEMBL804977

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

Binding
Displacement of [3H]citalopram from rat cortical serotonin transporter (SERT)
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Syntheses and binding affinities of 6-nitroquipazine analogues for serotonin transporter. Part 2: 4-substituted 6-nitroquipazines.
Se Lee B, Chu S, Lee BS, Yoon Chi D, Song YS, Jin C.
Bioorg Med Chem Lett (2002) 12 : 811 -815
PubMed 11859009 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 8.67 10.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL23034 1 10.89
CHEMBL423269 1 10.52
CHEMBL41140 6-NITROQUIPAZINE 1 9.77
CHEMBL166280 1 9.49
CHEMBL167825 1 9.43
CHEMBL490 PAROXETINE 4.0 1 9.28
CHEMBL167358 1 8.78
CHEMBL167475 1 8.76
CHEMBL166870 1 8.74
CHEMBL166948 1 8.28
CHEMBL41 FLUOXETINE 4.0 1 7.66
CHEMBL167487 1 7.22
CHEMBL353780 1 7.21
CHEMBL436441 1 7.17
CHEMBL422203 1 6.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL23034 Ki = 0.013 nM 10.89
CHEMBL423269 Ki = 0.03 nM 10.52
CHEMBL41140 6-NITROQUIPAZINE Ki = 0.17 nM 9.77
CHEMBL166280 Ki = 0.32 nM 9.49
CHEMBL167825 Ki = 0.37 nM 9.43
CHEMBL490 PAROXETINE Ki = 0.53 nM 9.28
CHEMBL167358 Ki = 1.67 nM 8.78
CHEMBL167475 Ki = 1.73 nM 8.76
CHEMBL166870 Ki = 1.82 nM 8.74
CHEMBL166948 Ki = 5.23 nM 8.28
CHEMBL41 FLUOXETINE Ki = 22.13 nM 7.66
CHEMBL167487 Ki = 60.03 nM 7.22
CHEMBL353780 Ki = 61.12 nM 7.21
CHEMBL436441 Ki = 67.24 nM 7.17
CHEMBL422203 Ki = 126.86 nM 6.90