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Assay Detail

CHEMBL4343397

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

Binding
Antagonist activity at 5-HT1A receptor (unknown origin)
22
Total Activities
22
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 1A (CHEMBL214)
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 21 6.58 8.19
IC50 1 6.30 6.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4205783 JNJ-18038683 FREE BASE 2.0 1 8.19
CHEMBL161765 1 7.80
CHEMBL2164327 1 7.05
CHEMBL3302600 1 6.92
CHEMBL4533865 1 6.89
CHEMBL69257 1 6.77
CHEMBL427518 1 6.57
CHEMBL348890 1 6.50
CHEMBL2164336 1 6.32
CHEMBL4582321 1 6.30
CHEMBL4521657 1 6.25
CHEMBL3139441 1 6.16
CHEMBL4205349 1 6.16
CHEMBL12624 SB-258741 1 6.00
CHEMBL409662 1 5.79
CHEMBL232791 1 5.32
CHEMBL282199 1 -
CHEMBL12264 SB-258719 1 -
CHEMBL182797 1 -
CHEMBL182322 1 -
CHEMBL3321794 1 -
CHEMBL4216782 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4205783 JNJ-18038683 FREE BASE Ki = 6.5 nM 8.19
CHEMBL161765 Ki = 16.0 nM 7.80
CHEMBL2164327 Ki = 89.7 nM 7.05
CHEMBL3302600 Ki = 121.0 nM 6.92
CHEMBL4533865 Ki = 128.0 nM 6.89
CHEMBL69257 Ki = 169.0 nM 6.77
CHEMBL427518 Ki = 272.0 nM 6.57
CHEMBL348890 Ki = 316.0 nM 6.50
CHEMBL2164336 Ki = 476.0 nM 6.32
CHEMBL4582321 IC50 = 500.0 nM 6.30
CHEMBL4521657 Ki = 562.0 nM 6.25
CHEMBL3139441 Ki = 700.0 nM 6.16
CHEMBL4205349 Ki = 700.0 nM 6.16
CHEMBL12624 SB-258741 Ki = 1000.0 nM 6.00
CHEMBL409662 Ki = 1610.0 nM 5.79
CHEMBL232791 Ki = 4826.0 nM 5.32
CHEMBL282199 Ki > 10000.0 nM -
CHEMBL12264 SB-258719 Ki > 3000.0 nM -
CHEMBL182797 Ki > 100.0 nM -
CHEMBL182322 Ki > 100.0 nM -
CHEMBL3321794 Ki > 1000.0 nM -
CHEMBL4216782 Ki > 10000.0 nM -