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Assay Detail

CHEMBL828658

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Binding
Inhibition of 8-OH DPAT binding to rat hydroxytryptamine 1A receptor expressed in CHO cells
ChEMBL ↗
51
Total Activities
50
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 1A (CHEMBL273) ↗
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 51 8.44 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL189704 — — 1 10.00
CHEMBL363055 — — 1 9.70
CHEMBL364592 — — 1 9.70
CHEMBL439849 VILAZODONE 4.0 2 9.52
CHEMBL184556 — — 1 9.40
CHEMBL185730 — — 1 9.40
CHEMBL188296 — — 1 9.30
CHEMBL188848 — — 1 9.22
CHEMBL278471 — — 1 9.15
CHEMBL188799 — — 1 9.15
CHEMBL185768 — — 1 9.15
CHEMBL359566 — — 1 9.00
CHEMBL189758 — — 1 9.00
CHEMBL427523 — — 1 9.00
CHEMBL189709 — — 1 9.00
CHEMBL186424 — — 1 8.96
CHEMBL188834 — — 1 8.85
CHEMBL189759 — — 1 8.80
CHEMBL188530 — — 1 8.72
CHEMBL188409 — — 1 8.70
CHEMBL189033 — — 1 8.70
CHEMBL186468 — — 1 8.70
CHEMBL360390 — — 1 8.52
CHEMBL185764 — — 1 8.51
CHEMBL184171 — — 1 8.49
CHEMBL186138 — — 1 8.48
CHEMBL188833 — — 1 8.40
CHEMBL185631 — — 1 8.40
CHEMBL188798 — — 1 8.40
CHEMBL186219 — — 1 8.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL189704 — IC50 = 0.1 nM 10.00
CHEMBL363055 — IC50 = 0.2 nM 9.70
CHEMBL364592 — IC50 = 0.2 nM 9.70
CHEMBL439849 VILAZODONE IC50 = 0.3 nM 9.52
CHEMBL185730 — IC50 = 0.4 nM 9.40
CHEMBL184556 — IC50 = 0.4 nM 9.40
CHEMBL188296 — IC50 = 0.5 nM 9.30
CHEMBL188848 — IC50 = 0.6 nM 9.22
CHEMBL278471 — IC50 = 0.7 nM 9.15
CHEMBL188799 — IC50 = 0.7 nM 9.15
CHEMBL185768 — IC50 = 0.7 nM 9.15
CHEMBL189758 — IC50 = 1.0 nM 9.00
CHEMBL427523 — IC50 = 1.0 nM 9.00
CHEMBL359566 — IC50 = 1.0 nM 9.00
CHEMBL189709 — IC50 = 1.0 nM 9.00
CHEMBL186424 — IC50 = 1.1 nM 8.96
CHEMBL188834 — IC50 = 1.4 nM 8.85
CHEMBL189759 — IC50 = 1.6 nM 8.80
CHEMBL188530 — IC50 = 1.9 nM 8.72
CHEMBL188409 — IC50 = 2.0 nM 8.70
CHEMBL189033 — IC50 = 2.0 nM 8.70
CHEMBL186468 — IC50 = 2.0 nM 8.70
CHEMBL360390 — IC50 = 3.0 nM 8.52
CHEMBL185764 — IC50 = 3.1 nM 8.51
CHEMBL184171 — IC50 = 3.2 nM 8.49
CHEMBL186138 — IC50 = 3.3 nM 8.48
CHEMBL185631 — IC50 = 4.0 nM 8.40
CHEMBL188798 — IC50 = 4.0 nM 8.40
CHEMBL188833 — IC50 = 4.0 nM 8.40
CHEMBL439849 VILAZODONE IC50 = 4.4 nM 8.36
CHEMBL186655 — IC50 = 5.0 nM 8.30
CHEMBL186219 — IC50 = 5.0 nM 8.30
CHEMBL188481 — IC50 = 5.0 nM 8.30
CHEMBL433968 — IC50 = 5.6 nM 8.25
CHEMBL186654 — IC50 = 6.0 nM 8.22
CHEMBL189722 — IC50 = 6.4 nM 8.19
CHEMBL185805 — IC50 = 8.0 nM 8.10
CHEMBL364610 — IC50 = 8.0 nM 8.10
CHEMBL184343 — IC50 = 8.7 nM 8.06
CHEMBL364846 — IC50 = 12.0 nM 7.92
CHEMBL365643 — IC50 = 14.0 nM 7.85
CHEMBL366300 — IC50 = 14.0 nM 7.85
CHEMBL426067 — IC50 = 30.0 nM 7.52
CHEMBL189553 — IC50 = 36.0 nM 7.44
CHEMBL189869 — IC50 = 40.0 nM 7.40
CHEMBL185807 — IC50 = 40.0 nM 7.40
CHEMBL360407 — IC50 = 40.0 nM 7.40
CHEMBL184162 — IC50 = 60.0 nM 7.22
CHEMBL187909 — IC50 = 118.0 nM 6.93
CHEMBL188835 — IC50 = 400.0 nM 6.40