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Assay Detail

CHEMBL809443

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

Binding
In vitro binding affinity towards serotonin transporter using [3H]citalopram as radioligand in rat cerebral cortex membranes
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Cerebral cortex
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

SAR development of a selective 5-HT1D antagonist/serotonin reuptake inhibitor lead using rapid parallel synthesis.
Timms GH, Boot JR, Broadmore RJ, Carney SL, Cooper J, Findlay JD, Gilmore J, Mitchell S, Moore NA, Pullar I, Sanger GJ, Tomlinson R, Tree BB, Wedley S.
Bioorg Med Chem Lett (2004) 14 : 2469 -2472
PubMed 15109634 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 27 8.85 9.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL83617 1 9.96
CHEMBL1159649 1 9.70
CHEMBL84305 1 9.55
CHEMBL82488 1 9.54
CHEMBL82523 1 9.52
CHEMBL1169435 1 9.52
CHEMBL309872 1 9.42
CHEMBL441259 1 9.30
CHEMBL442974 1 9.27
CHEMBL83112 1 9.12
CHEMBL311787 1 9.11
CHEMBL311323 1 9.01
CHEMBL81703 1 9.00
CHEMBL313452 1 9.00
CHEMBL79561 1 8.80
CHEMBL2112307 1 8.72
CHEMBL79674 1 8.70
CHEMBL79725 1 8.68
CHEMBL311694 1 8.68
CHEMBL310082 1 8.66
CHEMBL81191 1 8.49
CHEMBL84171 1 8.46
CHEMBL79853 1 8.10
CHEMBL83732 1 7.89
CHEMBL79693 1 7.82
CHEMBL310744 1 7.72
CHEMBL444843 1 7.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL83617 Ki = 0.11 nM 9.96
CHEMBL1159649 Ki = 0.2 nM 9.70
CHEMBL84305 Ki = 0.28 nM 9.55
CHEMBL82488 Ki = 0.29 nM 9.54
CHEMBL82523 Ki = 0.3 nM 9.52
CHEMBL1169435 Ki = 0.3 nM 9.52
CHEMBL309872 Ki = 0.38 nM 9.42
CHEMBL441259 Ki = 0.5 nM 9.30
CHEMBL442974 Ki = 0.54 nM 9.27
CHEMBL83112 Ki = 0.76 nM 9.12
CHEMBL311787 Ki = 0.78 nM 9.11
CHEMBL311323 Ki = 0.98 nM 9.01
CHEMBL81703 Ki = 1.0 nM 9.00
CHEMBL313452 Ki = 0.99 nM 9.00
CHEMBL79561 Ki = 1.6 nM 8.80
CHEMBL2112307 Ki = 1.9 nM 8.72
CHEMBL79674 Ki = 2.0 nM 8.70
CHEMBL79725 Ki = 2.1 nM 8.68
CHEMBL311694 Ki = 2.1 nM 8.68
CHEMBL310082 Ki = 2.2 nM 8.66
CHEMBL81191 Ki = 3.2 nM 8.49
CHEMBL84171 Ki = 3.5 nM 8.46
CHEMBL79853 Ki = 8.0 nM 8.10
CHEMBL83732 Ki = 13.0 nM 7.89
CHEMBL79693 Ki = 15.0 nM 7.82
CHEMBL310744 Ki = 19.0 nM 7.72
CHEMBL444843 Ki = 53.0 nM 7.28