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Assay Detail

CHEMBL1260567

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

Binding
Displacement of [3H]-citalopram from human serotonin transporter expressed in HEK 293 cells
37
Total Activities
37
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

6-Alkoxyisoindolin-1-one based dopamine D2 partial agonists as potential antipsychotics.
Favor DA, Powers JJ, White AD, Fitzgerald LW, Groppi V, Serpa KA.
Bioorg Med Chem Lett (2010) 20 : 5666 -5669
PubMed 20801650 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 37 7.14 8.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1258881 1 8.04
CHEMBL1258649 1 7.98
CHEMBL1258650 1 7.87
CHEMBL1258535 1 7.81
CHEMBL1258647 1 7.78
CHEMBL1258763 1 7.65
CHEMBL1258879 1 7.58
CHEMBL1258534 1 7.51
CHEMBL1258314 1 7.43
CHEMBL1258428 1 7.26
CHEMBL1258199 1 7.24
CHEMBL1257969 1 7.07
CHEMBL1258762 1 6.96
CHEMBL1258085 1 6.80
CHEMBL1258313 1 6.59
CHEMBL1258200 1 5.75
CHEMBL1258084 1 5.60
CHEMBL1258427 1 5.57
CHEMBL1258087 1 -
CHEMBL1258086 1 -
CHEMBL1257971 1 -
CHEMBL1257970 1 -
CHEMBL1257859 1 -
CHEMBL1257858 1 -
CHEMBL1257737 1 -
CHEMBL1257736 1 -
CHEMBL1257616 1 -
CHEMBL1257615 1 -
CHEMBL1257495 1 -
CHEMBL1257494 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1258881 Ki = 9.1 nM 8.04
CHEMBL1258649 Ki = 10.5 nM 7.98
CHEMBL1258650 Ki = 13.6 nM 7.87
CHEMBL1258535 Ki = 15.6 nM 7.81
CHEMBL1258647 Ki = 16.5 nM 7.78
CHEMBL1258763 Ki = 22.2 nM 7.65
CHEMBL1258879 Ki = 26.0 nM 7.58
CHEMBL1258534 Ki = 30.8 nM 7.51
CHEMBL1258314 Ki = 37.4 nM 7.43
CHEMBL1258428 Ki = 54.6 nM 7.26
CHEMBL1258199 Ki = 57.2 nM 7.24
CHEMBL1257969 Ki = 84.7 nM 7.07
CHEMBL1258762 Ki = 110.0 nM 6.96
CHEMBL1258085 Ki = 160.0 nM 6.80
CHEMBL1258313 Ki = 259.0 nM 6.59
CHEMBL1258200 Ki = 1770.0 nM 5.75
CHEMBL1258084 Ki = 2520.0 nM 5.60
CHEMBL1258427 Ki = 2720.0 nM 5.57
CHEMBL1258882 Ki - -
CHEMBL1257146 Ki - -
CHEMBL1257147 Ki - -
CHEMBL1257263 Ki - -
CHEMBL1257264 Ki - -
CHEMBL1257384 Ki - -
CHEMBL1257385 Ki - -
CHEMBL1257494 Ki - -
CHEMBL1257495 Ki - -
CHEMBL1257615 Ki - -
CHEMBL1257616 Ki - -
CHEMBL1257736 Ki - -
CHEMBL1257737 Ki - -
CHEMBL1257858 Ki - -
CHEMBL1257859 Ki - -
CHEMBL1257970 Ki - -
CHEMBL1257971 Ki - -
CHEMBL1258086 Ki - -
CHEMBL1258087 Ki - -