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Assay Detail

CHEMBL3877018

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

Binding
Displacement of [3H]-5-HT from recombinant human 5-HT7A receptor expressed in CHOK1 cell membranes after 40 mins by liquid scintillation counting method
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

New N- and O-arylpiperazinylalkyl pyrimidines and 2-methylquinazolines derivatives as 5-HT7 and 5-HT1A receptor ligands: Synthesis, structure-activity relationships, and molecular modeling studies.
Intagliata S, Modica MN, Pittalà V, Salerno L, Siracusa MA, Cagnotto A, Salmona M, Kurczab R, Romeo G.
Bioorg Med Chem (2017) 25 : 1250 -1259
PubMed 28063784 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 6.90 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL282199 1 9.15
CHEMBL3884095 1 8.07
CHEMBL3883640 1 7.63
CHEMBL3883542 1 7.46
CHEMBL3884778 1 7.35
CHEMBL3884714 1 7.35
CHEMBL3885389 1 7.27
CHEMBL3884584 1 7.02
CHEMBL3885319 1 6.84
CHEMBL3883995 1 6.74
CHEMBL3883517 1 6.56
CHEMBL3885178 1 6.49
CHEMBL56 8-OH-DPAT 1 6.41
CHEMBL3884137 1 6.21
CHEMBL3884743 1 6.00
CHEMBL3884728 1 5.88
CHEMBL3884634 1 5.88
CHEMBL3885282 1 5.86

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL282199 Ki = 0.71 nM 9.15
CHEMBL3884095 Ki = 8.42 nM 8.07
CHEMBL3883640 Ki = 23.5 nM 7.63
CHEMBL3883542 Ki = 35.1 nM 7.46
CHEMBL3884778 Ki = 45.1 nM 7.35
CHEMBL3884714 Ki = 44.8 nM 7.35
CHEMBL3885389 Ki = 53.7 nM 7.27
CHEMBL3884584 Ki = 94.7 nM 7.02
CHEMBL3885319 Ki = 143.0 nM 6.84
CHEMBL3883995 Ki = 181.0 nM 6.74
CHEMBL3883517 Ki = 276.0 nM 6.56
CHEMBL3885178 Ki = 327.0 nM 6.49
CHEMBL56 8-OH-DPAT Ki = 388.0 nM 6.41
CHEMBL3884137 Ki = 613.0 nM 6.21
CHEMBL3884743 Ki = 990.0 nM 6.00
CHEMBL3884728 Ki = 1310.0 nM 5.88
CHEMBL3884634 Ki = 1328.0 nM 5.88
CHEMBL3885282 Ki = 1377.0 nM 5.86