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Assay Detail

CHEMBL4770539

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

Binding
Displacement of [3H]-5-CT from human 5-HT7R expressed in human HEK293 cells assessed as inhibitory constant incubated for 60 mins by radioligand binding assay
22
Total Activities
22
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

Privileged scaffold-based design to identify a novel drug-like 5-HT receptor-preferring agonist to target Fragile X syndrome.
Lacivita E,Niso M,Stama ML,Arzuaga A,Altamura C,Costa L,Desaphy JF,Ragozzino ME,Ciranna L,Leopoldo M
Eur J Med Chem (2020) 199 : 112395 -112395
PubMed 32442850 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 7.57 9.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL18840 1 9.46
CHEMBL4781863 1 7.88
CHEMBL4799274 1 7.83
CHEMBL4789865 1 7.82
CHEMBL4794688 1 7.80
CHEMBL4780452 1 7.79
CHEMBL4783043 1 7.75
CHEMBL4795056 1 7.70
CHEMBL4785158 1 7.63
CHEMBL4791805 1 7.60
CHEMBL4797980 1 7.59
CHEMBL4792307 1 7.58
CHEMBL4778946 1 7.45
CHEMBL4782879 1 7.44
CHEMBL4784089 1 7.37
CHEMBL4788259 1 7.35
CHEMBL4793310 1 7.34
CHEMBL4779459 1 7.33
CHEMBL4777209 1 7.21
CHEMBL4784167 1 7.20
CHEMBL4781056 1 7.13
CHEMBL4798874 1 6.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL18840 Ki = 0.35 nM 9.46
CHEMBL4781863 Ki = 13.2 nM 7.88
CHEMBL4799274 Ki = 14.7 nM 7.83
CHEMBL4789865 Ki = 15.2 nM 7.82
CHEMBL4794688 Ki = 15.7 nM 7.80
CHEMBL4780452 Ki = 16.1 nM 7.79
CHEMBL4783043 Ki = 17.7 nM 7.75
CHEMBL4795056 Ki = 19.9 nM 7.70
CHEMBL4785158 Ki = 23.6 nM 7.63
CHEMBL4791805 Ki = 25.1 nM 7.60
CHEMBL4797980 Ki = 25.7 nM 7.59
CHEMBL4792307 Ki = 26.5 nM 7.58
CHEMBL4778946 Ki = 35.8 nM 7.45
CHEMBL4782879 Ki = 36.0 nM 7.44
CHEMBL4784089 Ki = 42.9 nM 7.37
CHEMBL4788259 Ki = 44.3 nM 7.35
CHEMBL4793310 Ki = 45.8 nM 7.34
CHEMBL4779459 Ki = 47.3 nM 7.33
CHEMBL4777209 Ki = 61.4 nM 7.21
CHEMBL4784167 Ki = 62.8 nM 7.20
CHEMBL4781056 Ki = 74.5 nM 7.13
CHEMBL4798874 Ki = 410.0 nM 6.39