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Assay Detail

CHEMBL4343396

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

Binding
Antagonist activity at 5-HT7 receptor (unknown origin)
21
Total Activities
21
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Structure-activity relationships of serotonin 5-HT<sub>7</sub> receptors ligands: A review.
Thirumaran SL, Lepailleur A, Rochais C.
Eur J Med Chem (2019) 183 : 111705 -111705
PubMed 31581003 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 8.58 9.33
IC50 1 7.92 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4216782 1 9.33
CHEMBL161765 1 9.22
CHEMBL2164327 1 9.22
CHEMBL3321794 1 9.15
CHEMBL409662 1 9.10
CHEMBL282199 1 8.90
CHEMBL4521657 1 8.70
CHEMBL182322 1 8.70
CHEMBL69257 1 8.67
CHEMBL4205349 1 8.60
CHEMBL2164336 1 8.59
CHEMBL3302600 1 8.52
CHEMBL182797 1 8.52
CHEMBL12624 SB-258741 1 8.49
CHEMBL4533865 1 8.45
CHEMBL3139441 1 8.35
CHEMBL348890 1 8.14
CHEMBL232791 1 8.07
CHEMBL4582321 1 7.92
CHEMBL12264 SB-258719 1 7.50
CHEMBL427518 1 7.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4216782 Ki = 0.47 nM 9.33
CHEMBL161765 Ki = 0.6 nM 9.22
CHEMBL2164327 Ki = 0.6 nM 9.22
CHEMBL3321794 Ki = 0.7 nM 9.15
CHEMBL409662 Ki = 0.79 nM 9.10
CHEMBL282199 Ki = 1.25 nM 8.90
CHEMBL4521657 Ki = 1.99 nM 8.70
CHEMBL182322 Ki = 2.0 nM 8.70
CHEMBL69257 Ki = 2.13 nM 8.67
CHEMBL4205349 Ki = 2.5 nM 8.60
CHEMBL2164336 Ki = 2.6 nM 8.59
CHEMBL3302600 Ki = 3.0 nM 8.52
CHEMBL182797 Ki = 3.0 nM 8.52
CHEMBL12624 SB-258741 Ki = 3.2 nM 8.49
CHEMBL4533865 Ki = 3.54 nM 8.45
CHEMBL3139441 Ki = 4.5 nM 8.35
CHEMBL348890 Ki = 7.24 nM 8.14
CHEMBL232791 Ki = 8.6 nM 8.07
CHEMBL4582321 IC50 = 12.0 nM 7.92
CHEMBL12264 SB-258719 Ki = 31.6 nM 7.50
CHEMBL427518 Ki = 37.0 nM 7.43