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Assay Detail

CHEMBL1072174

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

Binding
Displacement of [3H]5CT from human cloned 5HT7B receptor expressed in HEK293 cells
25
Total Activities
25
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

SAR studies on new bis-aryls 5-HT7 ligands: Synthesis and molecular modeling.
Badarau E, Bugno R, Suzenet F, Bojarski AJ, Finaru AL, Guillaumet G.
Bioorg Med Chem (2010) 18 : 1958 -1967
PubMed 20138771 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 25 7.22 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL596959 1 9.52
CHEMBL158402 1 9.15
CHEMBL183329 1 8.59
CHEMBL362540 1 8.54
CHEMBL186112 1 8.47
CHEMBL161765 1 8.21
CHEMBL395870 1 8.12
CHEMBL345803 1 7.92
CHEMBL367584 1 7.87
CHEMBL599612 1 7.58
CHEMBL158285 1 7.43
CHEMBL597357 1 6.89
CHEMBL20666 1 6.81
CHEMBL607584 1 6.26
CHEMBL599819 1 6.17
CHEMBL584429 1 5.84
CHEMBL608138 1 5.83
CHEMBL589524 1 5.79
CHEMBL597356 1 5.65
CHEMBL599818 1 5.58
CHEMBL610515 1 5.39
CHEMBL596958 1 -
CHEMBL599000 1 -
CHEMBL603062 1 -
CHEMBL590501 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL596959 Ki = 0.3 nM 9.52
CHEMBL158402 Ki = 0.7 nM 9.15
CHEMBL183329 Ki = 2.55 nM 8.59
CHEMBL362540 Ki = 2.91 nM 8.54
CHEMBL186112 Ki = 3.38 nM 8.47
CHEMBL161765 Ki = 6.2 nM 8.21
CHEMBL395870 Ki = 7.6 nM 8.12
CHEMBL345803 Ki = 12.0 nM 7.92
CHEMBL367584 Ki = 13.4 nM 7.87
CHEMBL599612 Ki = 26.0 nM 7.58
CHEMBL158285 Ki = 37.0 nM 7.43
CHEMBL597357 Ki = 128.0 nM 6.89
CHEMBL20666 Ki = 156.0 nM 6.81
CHEMBL607584 Ki = 553.0 nM 6.26
CHEMBL599819 Ki = 669.0 nM 6.17
CHEMBL584429 Ki = 1429.0 nM 5.84
CHEMBL608138 Ki = 1485.0 nM 5.83
CHEMBL589524 Ki = 1614.0 nM 5.79
CHEMBL597356 Ki = 2240.0 nM 5.65
CHEMBL599818 Ki = 2663.0 nM 5.58
CHEMBL610515 Ki = 4110.0 nM 5.39
CHEMBL596958 Ki > 10000.0 nM -
CHEMBL599000 Ki > 10000.0 nM -
CHEMBL603062 Ki > 10000.0 nM -
CHEMBL590501 Ki > 10000.0 nM -