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Assay Detail

CHEMBL830976

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

Binding
Inhibition of [3H]5-HT re-uptake in rat synaptosomes
ChEMBL ↗
50
Total Activities
49
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and structure--activity relationship in a class of indolebutylpiperazines as dual 5-HT(1A) receptor agonists and serotonin reuptake inhibitors.
Heinrich T, Böttcher H, Gericke R, Bartoszyk GD, Anzali S, Seyfried CA, Greiner HE, Van Amsterdam C.
J Med Chem (2004) 47 : 4684 -4692
PubMed 15341484 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 50 8.68 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL184162 — — 1 9.52
CHEMBL185764 — — 1 9.52
CHEMBL360390 — — 1 9.52
CHEMBL189709 — — 1 9.40
CHEMBL363055 — — 1 9.30
CHEMBL186654 — — 1 9.30
CHEMBL189758 — — 1 9.30
CHEMBL439849 VILAZODONE 4.0 2 9.30
CHEMBL188799 — — 1 9.22
CHEMBL187909 — — 1 9.22
CHEMBL189704 — — 1 9.15
CHEMBL363754 — — 1 9.10
CHEMBL278471 — — 1 9.05
CHEMBL188481 — — 1 9.05
CHEMBL188835 — — 1 9.00
CHEMBL185631 — — 1 9.00
CHEMBL186655 — — 1 9.00
CHEMBL188409 — — 1 9.00
CHEMBL188798 — — 1 9.00
CHEMBL184556 — — 1 9.00
CHEMBL185768 — — 1 9.00
CHEMBL186424 — — 1 8.89
CHEMBL359566 — — 1 8.82
CHEMBL189869 — — 1 8.70
CHEMBL364846 — — 1 8.70
CHEMBL366300 — — 1 8.70
CHEMBL185807 — — 1 8.70
CHEMBL189759 — — 1 8.62
CHEMBL188530 — — 1 8.59
CHEMBL427523 — — 1 8.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL360390 — IC50 = 0.3 nM 9.52
CHEMBL184162 — IC50 = 0.3 nM 9.52
CHEMBL185764 — IC50 = 0.3 nM 9.52
CHEMBL189709 — IC50 = 0.4 nM 9.40
CHEMBL189758 — IC50 = 0.5 nM 9.30
CHEMBL186654 — IC50 = 0.5 nM 9.30
CHEMBL439849 VILAZODONE IC50 = 0.5 nM 9.30
CHEMBL363055 — IC50 = 0.5 nM 9.30
CHEMBL187909 — IC50 = 0.6 nM 9.22
CHEMBL188799 — IC50 = 0.6 nM 9.22
CHEMBL189704 — IC50 = 0.7 nM 9.15
CHEMBL363754 — IC50 = 0.8 nM 9.10
CHEMBL188481 — IC50 = 0.9 nM 9.05
CHEMBL278471 — IC50 = 0.9 nM 9.05
CHEMBL185631 — IC50 = 1.0 nM 9.00
CHEMBL186655 — IC50 = 1.0 nM 9.00
CHEMBL185768 — IC50 = 1.0 nM 9.00
CHEMBL188835 — IC50 = 1.0 nM 9.00
CHEMBL188409 — IC50 = 1.0 nM 9.00
CHEMBL188798 — IC50 = 1.0 nM 9.00
CHEMBL184556 — IC50 = 1.0 nM 9.00
CHEMBL439849 VILAZODONE IC50 = 1.1 nM 8.96
CHEMBL186424 — IC50 = 1.3 nM 8.89
CHEMBL359566 — IC50 = 1.5 nM 8.82
CHEMBL366300 — IC50 = 2.0 nM 8.70
CHEMBL189869 — IC50 = 2.0 nM 8.70
CHEMBL364846 — IC50 = 2.0 nM 8.70
CHEMBL185807 — IC50 = 2.0 nM 8.70
CHEMBL189759 — IC50 = 2.4 nM 8.62
CHEMBL188530 — IC50 = 2.6 nM 8.59
CHEMBL427523 — IC50 = 3.0 nM 8.52
CHEMBL186219 — IC50 = 3.0 nM 8.52
CHEMBL189033 — IC50 = 3.1 nM 8.51
CHEMBL184171 — IC50 = 3.1 nM 8.51
CHEMBL186468 — IC50 = 3.2 nM 8.49
CHEMBL365643 — IC50 = 3.4 nM 8.47
CHEMBL433968 — IC50 = 3.9 nM 8.41
CHEMBL184343 — IC50 = 3.9 nM 8.41
CHEMBL185805 — IC50 = 4.1 nM 8.39
CHEMBL185730 — IC50 = 5.0 nM 8.30
CHEMBL189553 — IC50 = 5.4 nM 8.27
CHEMBL186138 — IC50 = 5.5 nM 8.26
CHEMBL426067 — IC50 = 6.8 nM 8.17
CHEMBL188834 — IC50 = 8.5 nM 8.07
CHEMBL364610 — IC50 = 10.0 nM 8.00
CHEMBL189722 — IC50 = 16.0 nM 7.80
CHEMBL360407 — IC50 = 20.0 nM 7.70
CHEMBL188848 — IC50 = 50.0 nM 7.30
CHEMBL364592 — IC50 = 60.0 nM 7.22
CHEMBL188296 — IC50 = 100.0 nM 7.00