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Assay Detail

CHEMBL3240654

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

Binding
Displacement of [3H]-5-CT from human recombinant 5-HT7 receptor expressed in HEK293 cell membrane after 1 hr by Microbeta scintillation counting analysis
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 7 (CHEMBL3155)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

SAR-studies on the importance of aromatic ring topologies in search for selective 5-HT(7) receptor ligands among phenylpiperazine hydantoin derivatives.
Handzlik J, Bojarski AJ, Satała G, Kubacka M, Sadek B, Ashoor A, Siwek A, Więcek M, Kucwaj K, Filipek B, Kieć-Kononowicz K.
Eur J Med Chem (2014) 78 : 324 -339
PubMed 24691057 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 7.14 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3233679 1 8.52
CHEMBL2079256 1 7.80
CHEMBL42 CLOZAPINE 4.0 1 7.60
CHEMBL3233676 1 7.51
CHEMBL3233667 1 7.47
CHEMBL3233672 1 7.35
CHEMBL3233675 1 7.34
CHEMBL3233668 1 7.16
CHEMBL3233669 1 7.14
CHEMBL3233677 1 7.11
CHEMBL3233402 1 7.11
CHEMBL3233401 1 7.02
CHEMBL3233670 1 6.91
CHEMBL3233674 1 6.91
CHEMBL3233671 1 6.87
CHEMBL3233666 1 6.80
CHEMBL3233673 1 6.76
CHEMBL1916745 1 6.68
CHEMBL1916746 1 6.45
CHEMBL3233678 1 6.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3233679 Ki = 3.0 nM 8.52
CHEMBL2079256 Ki = 16.0 nM 7.80
CHEMBL42 CLOZAPINE Ki = 25.0 nM 7.60
CHEMBL3233676 Ki = 31.0 nM 7.51
CHEMBL3233667 Ki = 34.0 nM 7.47
CHEMBL3233672 Ki = 45.0 nM 7.35
CHEMBL3233675 Ki = 46.0 nM 7.34
CHEMBL3233668 Ki = 70.0 nM 7.16
CHEMBL3233669 Ki = 72.0 nM 7.14
CHEMBL3233677 Ki = 78.0 nM 7.11
CHEMBL3233402 Ki = 77.0 nM 7.11
CHEMBL3233401 Ki = 95.0 nM 7.02
CHEMBL3233670 Ki = 122.0 nM 6.91
CHEMBL3233674 Ki = 123.0 nM 6.91
CHEMBL3233671 Ki = 135.0 nM 6.87
CHEMBL3233666 Ki = 157.0 nM 6.80
CHEMBL3233673 Ki = 172.0 nM 6.76
CHEMBL1916745 Ki = 210.0 nM 6.68
CHEMBL1916746 Ki = 353.0 nM 6.45
CHEMBL3233678 Ki = 456.0 nM 6.34