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Assay Detail

CHEMBL806803

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

Binding
Affinity for RB Serotonin transporter was determined in vitro by incubating compound
10
Total Activities
10
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

Studies toward the discovery of the next generation of antidepressants. Part 2: incorporating a 5-HT(1A) antagonist component into a class of serotonin reuptake inhibitors.
Mewshaw RE, Meagher KL, Zhou P, Zhou D, Shi X, Scerni R, Smith D, Schechter LE, Andree TH.
Bioorg Med Chem Lett (2002) 12 : 307 -310
PubMed 11814784 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 9.28 11.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL106481 1 11.00
CHEMBL421027 1 10.52
CHEMBL105204 1 9.82
CHEMBL104144 1 9.77
CHEMBL318604 1 9.64
CHEMBL105390 1 8.93
CHEMBL104229 1 8.84
CHEMBL322915 1 8.33
CHEMBL442391 1 8.16
CHEMBL318738 1 7.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL106481 Ki = 0.01 nM 11.00
CHEMBL421027 Ki = 0.03 nM 10.52
CHEMBL105204 Ki = 0.15 nM 9.82
CHEMBL104144 Ki = 0.17 nM 9.77
CHEMBL318604 Ki = 0.23 nM 9.64
CHEMBL105390 Ki = 1.17 nM 8.93
CHEMBL104229 Ki = 1.46 nM 8.84
CHEMBL322915 Ki = 4.7 nM 8.33
CHEMBL442391 Ki = 6.89 nM 8.16
CHEMBL318738 Ki = 18.0 nM 7.75