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Assay Detail

CHEMBL785170

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

Functional
[3H]5-HT reuptake inhibition in Rat brain synaptosomes.
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Brain
Confidence 1 — Organism
Curated By Expert

Target

Rattus norvegicus (CHEMBL376)
Type ORGANISM
Organism Rattus norvegicus

Publication

5-HT reuptake inhibitors with 5-HT(1B/1D) antagonistic activity: a new approach toward efficient antidepressants.
Matzen L, van Amsterdam C, Rautenberg W, Greiner HE, Harting J, Seyfried CA, Böttcher H.
J Med Chem (2000) 43 : 1149 -1157
PubMed 10737747 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 7.65 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL276928 1 9.70
CHEMBL15837 1 9.15
CHEMBL279320 1 8.92
CHEMBL15965 1 8.72
CHEMBL430122 1 8.72
CHEMBL15909 1 8.66
CHEMBL280314 1 8.40
CHEMBL280000 1 8.00
CHEMBL2079627 1 7.68
CHEMBL278917 1 7.31
CHEMBL15961 1 7.19
CHEMBL279646 1 6.97
CHEMBL15855 1 6.70
CHEMBL15139 1 6.50
CHEMBL16035 1 6.41
CHEMBL15808 1 6.33
CHEMBL274922 1 6.33
CHEMBL15928 GR-127935 1 6.00
CHEMBL15933 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL276928 IC50 = 0.2 nM 9.70
CHEMBL15837 IC50 = 0.7 nM 9.15
CHEMBL279320 IC50 = 1.2 nM 8.92
CHEMBL15965 IC50 = 1.9 nM 8.72
CHEMBL430122 IC50 = 1.9 nM 8.72
CHEMBL15909 IC50 = 2.2 nM 8.66
CHEMBL280314 IC50 = 4.0 nM 8.40
CHEMBL280000 IC50 = 10.0 nM 8.00
CHEMBL2079627 IC50 = 21.0 nM 7.68
CHEMBL278917 IC50 = 49.0 nM 7.31
CHEMBL15961 IC50 = 65.0 nM 7.19
CHEMBL279646 IC50 = 106.0 nM 6.97
CHEMBL15855 IC50 = 200.0 nM 6.70
CHEMBL15139 IC50 = 314.0 nM 6.50
CHEMBL16035 IC50 = 387.0 nM 6.41
CHEMBL15808 IC50 = 469.0 nM 6.33
CHEMBL274922 IC50 = 472.0 nM 6.33
CHEMBL15928 GR-127935 IC50 = 1000.0 nM 6.00
CHEMBL15933 IC50 > 1000.0 nM -