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Assay Detail

CHEMBL5039770

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

Binding
Displacement of [3H] D-lysergic acid diethylamide from 5-HT7R (unknown origin) transfected in HEK293 cells incubated for 1.5 hrs by microbeta scintillation counter analysis
33
Total Activities
17
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

Discovery of G Protein-Biased Ligands against 5-HT<sub>7</sub>R.
Lee J, Kwag R, Lee S, Kim D, Woo J, Cho Y, Kim HJ, Kim J, Jeon B, Choo H.
J Med Chem (2021) 64 : 7453 -7467
PubMed 34032427 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 33 8.00 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4205349 2 8.89
CHEMBL5094234 2 8.80
CHEMBL5091373 2 8.80
CHEMBL5074190 2 8.60
CHEMBL5077293 2 8.56
CHEMBL3961059 2 8.28
CHEMBL5081379 2 8.20
CHEMBL5093342 2 8.07
CHEMBL5074880 2 8.03
CHEMBL3931889 2 7.75
CHEMBL5094493 2 7.70
CHEMBL5084249 2 7.60
CHEMBL5083607 2 7.52
CHEMBL5094680 2 7.28
CHEMBL5090884 2 7.19
CHEMBL5071978 2 7.00
CHEMBL5082177 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4205349 Ki = 1.3 nM 8.89
CHEMBL4205349 Ki = 1.288 nM 8.89
CHEMBL5094234 Ki = 1.585 nM 8.80
CHEMBL5091373 Ki = 1.6 nM 8.80
CHEMBL5074190 Ki = 2.5 nM 8.60
CHEMBL5074190 Ki = 2.512 nM 8.60
CHEMBL5077293 Ki = 2.754 nM 8.56
CHEMBL5077293 Ki = 2.8 nM 8.55
CHEMBL5091373 Ki = 2.818 nM 8.55
CHEMBL5094234 Ki = 2.8 nM 8.55
CHEMBL3961059 Ki = 5.248 nM 8.28
CHEMBL3961059 Ki = 5.2 nM 8.28
CHEMBL5081379 Ki = 6.31 nM 8.20
CHEMBL5081379 Ki = 6.8 nM 8.17
CHEMBL5093342 Ki = 8.511 nM 8.07
CHEMBL5093342 Ki = 8.7 nM 8.06
CHEMBL5074880 Ki = 9.3 nM 8.03
CHEMBL5074880 Ki = 10.0 nM 8.00
CHEMBL3931889 Ki = 18.0 nM 7.75
CHEMBL5094493 Ki = 19.95 nM 7.70
CHEMBL5094493 Ki = 20.0 nM 7.70
CHEMBL3931889 Ki = 19.95 nM 7.70
CHEMBL5084249 Ki = 25.12 nM 7.60
CHEMBL5084249 Ki = 25.0 nM 7.60
CHEMBL5083607 Ki = 30.2 nM 7.52
CHEMBL5083607 Ki = 30.0 nM 7.52
CHEMBL5094680 Ki = 52.0 nM 7.28
CHEMBL5094680 Ki = 52.48 nM 7.28
CHEMBL5090884 Ki = 64.57 nM 7.19
CHEMBL5090884 Ki = 64.0 nM 7.19
CHEMBL5071978 Ki = 100.0 nM 7.00
CHEMBL5071978 Ki = 110.0 nM 6.96
CHEMBL5082177 Ki > 10000.0 nM -