Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL5732165

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

Binding
5-HT1A Receptor Agonism Activity Test: The 5-HT1A receptor agonism activity test (The agonism activity of test compounds on 5-HT1A receptor expressing human recombinant 5-HT1A receptor in HEK293 cells) was performed using LANCE cAMP 384 Kit (Product of USA PerkinElmer Inc.). The 5-HT1A receptor agonism activity of test compounds was evaluated through their inhibition on cAMP production in HEK293 cells. cAMP concentration test was performed according to the method documented in the kit instructions. The concentration of the test compounds was 0.1 nM-10000 nM, 8-OH-DPAT was used as a positive control, EC50 value was calculated by the Excelfit software.
291
Total Activities
95
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 1A (CHEMBL214)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Heterocyclic compounds, process for preparation of the same and use thereof
(2019)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 97 8.22 9.65
kon 97 - -
k_off 97 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5909924 3 9.65
CHEMBL5774536 3 9.63
CHEMBL5975067 3 9.42
CHEMBL5792875 3 9.40
CHEMBL5874145 3 9.22
CHEMBL5766708 3 9.22
CHEMBL5839359 3 9.20
CHEMBL5830827 3 9.17
CHEMBL5742054 3 9.12
CHEMBL6060077 3 9.12
CHEMBL5925470 3 9.12
CHEMBL5945545 3 9.11
CHEMBL5792929 3 9.10
CHEMBL5810422 3 9.08
CHEMBL5771063 3 9.03
CHEMBL6035657 3 9.01
CHEMBL5849312 3 9.00
CHEMBL6045417 3 8.99
CHEMBL5804051 3 8.99
CHEMBL5995642 3 8.98
CHEMBL5916019 3 8.98
CHEMBL5856131 3 8.91
CHEMBL5900385 3 8.90
CHEMBL5836244 3 8.89
CHEMBL5770003 3 8.89
CHEMBL6045510 3 8.88
CHEMBL6007113 3 8.86
CHEMBL5984307 3 8.78
CHEMBL5763558 3 8.76
CHEMBL5762563 3 8.74

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5909924 EC50 = 0.223 nM 9.65
CHEMBL5774536 EC50 = 0.235 nM 9.63
CHEMBL5975067 EC50 = 0.379 nM 9.42
CHEMBL5792875 EC50 = 0.397 nM 9.40
CHEMBL5874145 EC50 = 0.602 nM 9.22
CHEMBL5766708 EC50 = 0.599 nM 9.22
CHEMBL5839359 EC50 = 0.626 nM 9.20
CHEMBL5830827 EC50 = 0.68 nM 9.17
CHEMBL6060077 EC50 = 0.761 nM 9.12
CHEMBL5925470 EC50 = 0.75 nM 9.12
CHEMBL5742054 EC50 = 0.766 nM 9.12
CHEMBL5945545 EC50 = 0.77 nM 9.11
CHEMBL5792929 EC50 = 0.787 nM 9.10
CHEMBL5810422 EC50 = 0.824 nM 9.08
CHEMBL5771063 EC50 = 0.926 nM 9.03
CHEMBL6035657 EC50 = 0.972 nM 9.01
CHEMBL5849312 EC50 = 1.01 nM 9.00
CHEMBL6045417 EC50 = 1.02 nM 8.99
CHEMBL5804051 EC50 = 1.02 nM 8.99
CHEMBL5916019 EC50 = 1.05 nM 8.98
CHEMBL5995642 EC50 = 1.05 nM 8.98
CHEMBL5856131 EC50 = 1.23 nM 8.91
CHEMBL5900385 EC50 = 1.25 nM 8.90
CHEMBL5770003 EC50 = 1.29 nM 8.89
CHEMBL5836244 EC50 = 1.29 nM 8.89
CHEMBL6045510 EC50 = 1.32 nM 8.88
CHEMBL6007113 EC50 = 1.38 nM 8.86
CHEMBL5984307 EC50 = 1.67 nM 8.78
CHEMBL5763558 EC50 = 1.74 nM 8.76
CHEMBL5762563 EC50 = 1.81 nM 8.74
CHEMBL5765721 EC50 = 1.95 nM 8.71
CHEMBL6058232 EC50 = 2.13 nM 8.67
CHEMBL5881637 EC50 = 2.24 nM 8.65
CHEMBL5904347 EC50 = 2.35 nM 8.63
CHEMBL6018186 EC50 = 2.53 nM 8.60
CHEMBL6048629 EC50 = 2.8 nM 8.55
CHEMBL5832082 EC50 = 2.9 nM 8.54
CHEMBL5807174 EC50 = 3.11 nM 8.51
CHEMBL5836576 EC50 = 3.29 nM 8.48
CHEMBL5949626 EC50 = 3.31 nM 8.48
CHEMBL6014626 EC50 = 4.5 nM 8.35
CHEMBL5914239 EC50 = 4.51 nM 8.35
CHEMBL4083333 EC50 = 4.57 nM 8.34
CHEMBL5891578 EC50 = 4.55 nM 8.34
CHEMBL5996307 EC50 = 4.8 nM 8.32
CHEMBL5885759 EC50 = 4.91 nM 8.31
CHEMBL6054287 EC50 = 5.64 nM 8.25
CHEMBL5979432 EC50 = 6.31 nM 8.20
CHEMBL5757494 EC50 = 6.3 nM 8.20
CHEMBL5865978 EC50 = 6.94 nM 8.16