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

CHEMBL4045106

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

Functional
Antagonist activity at 5-HT2A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 2A (CHEMBL224)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological investigation of tetrahydropyridopyrimidinone derivatives as potential multireceptor atypical antipsychotics.
Xiamuxi H, Wang Z, Li J, Wang Y, Wu C, Yang F, Jiang X, Liu Y, Zhao Q, Chen W, Zhang J, Xie Y, Hu T, Xu M, Guo S, Akber Aisa H, He Y, Shen J.
Bioorg Med Chem (2017) 25 : 4904 -4916
PubMed 28774576 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 37 7.57 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4083333 1 8.92
CHEMBL4098594 1 8.54
CHEMBL4102670 1 8.54
CHEMBL4061068 1 8.47
CHEMBL85 RISPERIDONE 4.0 1 8.33
CHEMBL4060678 1 8.29
CHEMBL4078409 1 8.29
CHEMBL1621 PALIPERIDONE 4.0 1 8.28
CHEMBL4084663 1 8.19
CHEMBL4096467 1 8.15
CHEMBL4094926 1 8.12
CHEMBL4094825 1 8.04
CHEMBL4065710 1 8.02
CHEMBL4082084 1 8.02
CHEMBL4077702 1 8.00
CHEMBL4104261 1 7.99
CHEMBL4087132 1 7.94
CHEMBL4079251 1 7.91
CHEMBL4062992 1 7.77
CHEMBL4090872 1 7.67
CHEMBL4062936 1 7.60
CHEMBL4097395 1 7.58
CHEMBL4087246 1 7.58
CHEMBL4079365 1 7.46
CHEMBL4074326 1 7.42
CHEMBL4103509 1 7.36
CHEMBL4101115 1 7.22
CHEMBL4091554 1 7.18
CHEMBL4102561 1 7.15
CHEMBL4074373 1 7.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4083333 IC50 = 1.19 nM 8.92
CHEMBL4098594 IC50 = 2.87 nM 8.54
CHEMBL4102670 IC50 = 2.9 nM 8.54
CHEMBL4061068 IC50 = 3.4 nM 8.47
CHEMBL85 RISPERIDONE IC50 = 4.67 nM 8.33
CHEMBL4060678 IC50 = 5.18 nM 8.29
CHEMBL4078409 IC50 = 5.12 nM 8.29
CHEMBL1621 PALIPERIDONE IC50 = 5.2 nM 8.28
CHEMBL4084663 IC50 = 6.4 nM 8.19
CHEMBL4096467 IC50 = 7.1 nM 8.15
CHEMBL4094926 IC50 = 7.66 nM 8.12
CHEMBL4094825 IC50 = 9.14 nM 8.04
CHEMBL4065710 IC50 = 9.49 nM 8.02
CHEMBL4082084 IC50 = 9.5 nM 8.02
CHEMBL4077702 IC50 = 10.0 nM 8.00
CHEMBL4104261 IC50 = 10.2 nM 7.99
CHEMBL4087132 IC50 = 11.5 nM 7.94
CHEMBL4079251 IC50 = 12.2 nM 7.91
CHEMBL4062992 IC50 = 17.0 nM 7.77
CHEMBL4090872 IC50 = 21.46 nM 7.67
CHEMBL4062936 IC50 = 25.0 nM 7.60
CHEMBL4097395 IC50 = 26.2 nM 7.58
CHEMBL4087246 IC50 = 26.4 nM 7.58
CHEMBL4079365 IC50 = 34.4 nM 7.46
CHEMBL4074326 IC50 = 37.6 nM 7.42
CHEMBL4103509 IC50 = 44.0 nM 7.36
CHEMBL4101115 IC50 = 60.0 nM 7.22
CHEMBL4091554 IC50 = 65.4 nM 7.18
CHEMBL4102561 IC50 = 71.3 nM 7.15
CHEMBL4074373 IC50 = 89.0 nM 7.05
CHEMBL4100152 IC50 = 244.0 nM 6.61
CHEMBL4077006 IC50 = 331.0 nM 6.48
CHEMBL4067506 IC50 = 651.0 nM 6.19
CHEMBL4063748 IC50 = 814.0 nM 6.09
CHEMBL4064609 IC50 = 1110.0 nM 5.96
CHEMBL4082150 IC50 = 1160.0 nM 5.94
CHEMBL4105102 IC50 = 2300.0 nM 5.64