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Assay Detail

CHEMBL4736130

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

ADMET
Displacement of [3H]-5-CT from human 5HT7b expressed in HEK293 cell membranes incubated for 1 hr by micro-beta plate reader based analysis
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Imidazopyridine-Based 5-HT Receptor Neutral Antagonists: Impact of N-Benzyl and N-Phenylsulfonyl Fragments on Different Receptor Conformational States.
Vanda D,Canale V,Chaumont-Dubel S,Kurczab R,Satała G,Koczurkiewicz-Adamczyk P,Krawczyk M,Pietruś W,Blicharz K,Pękala E,Bojarski AJ,Popik P,Marin P,Soural M,Zajdel P
J Med Chem (2021) 64 : 1180 -1196
PubMed 33439019 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 5.29 5.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4799851 1 5.51
CHEMBL4756814 1 5.42
CHEMBL4742804 1 5.41
CHEMBL4760105 1 5.37
CHEMBL4777550 1 5.18
CHEMBL1083390 INTEPIRDINE 3.0 1 4.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4799851 Ki = 3084.0 nM 5.51
CHEMBL4756814 Ki = 3763.0 nM 5.42
CHEMBL4742804 Ki = 3904.0 nM 5.41
CHEMBL4760105 Ki = 4300.0 nM 5.37
CHEMBL4777550 Ki = 6642.0 nM 5.18
CHEMBL1083390 INTEPIRDINE Ki = 14230.0 nM 4.85