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Assay Detail

CHEMBL958975

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

Binding
Displacement of [3H]LSD from human recombinant 5HT7 receptor expressed in CHO cell membrane
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Preparation of piperazine derivatives as 5-HT7 receptor antagonists.
Yoon J, Yoo EA, Kim JY, Pae AN, Rhim H, Park WK, Kong JY, Park Choo HY.
Bioorg Med Chem (2008) 16 : 5405 -5412
PubMed 18456500 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 6.65 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL495678 1 7.92
CHEMBL497749 1 7.70
CHEMBL427518 1 7.43
CHEMBL493816 1 7.33
CHEMBL495445 1 7.28
CHEMBL493625 1 7.05
CHEMBL492793 1 6.99
CHEMBL495250 1 6.97
CHEMBL495212 1 6.91
CHEMBL494428 1 6.85
CHEMBL493416 1 6.65
CHEMBL522006 1 6.54
CHEMBL493810 1 6.47
CHEMBL495685 1 6.43
CHEMBL523519 1 6.42
CHEMBL495890 1 6.42
CHEMBL494573 1 6.32
CHEMBL495884 1 6.25
CHEMBL493402 1 6.24
CHEMBL522694 1 6.17
CHEMBL492794 1 6.02
CHEMBL494427 1 5.49
CHEMBL493811 1 5.03
CHEMBL495677 1 -
CHEMBL497328 1 -
CHEMBL497327 1 -
CHEMBL493791 1 -
CHEMBL524007 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL495678 IC50 = 12.0 nM 7.92
CHEMBL497749 IC50 = 20.0 nM 7.70
CHEMBL427518 IC50 = 37.0 nM 7.43
CHEMBL493816 IC50 = 47.0 nM 7.33
CHEMBL495445 IC50 = 53.0 nM 7.28
CHEMBL493625 IC50 = 89.0 nM 7.05
CHEMBL492793 IC50 = 103.0 nM 6.99
CHEMBL495250 IC50 = 107.0 nM 6.97
CHEMBL495212 IC50 = 124.0 nM 6.91
CHEMBL494428 IC50 = 140.0 nM 6.85
CHEMBL493416 IC50 = 223.0 nM 6.65
CHEMBL522006 IC50 = 289.0 nM 6.54
CHEMBL493810 IC50 = 339.0 nM 6.47
CHEMBL495685 IC50 = 373.0 nM 6.43
CHEMBL523519 IC50 = 384.0 nM 6.42
CHEMBL495890 IC50 = 377.0 nM 6.42
CHEMBL494573 IC50 = 476.0 nM 6.32
CHEMBL495884 IC50 = 567.0 nM 6.25
CHEMBL493402 IC50 = 580.0 nM 6.24
CHEMBL522694 IC50 = 681.0 nM 6.17
CHEMBL492794 IC50 = 949.0 nM 6.02
CHEMBL494427 IC50 = 3241.0 nM 5.49
CHEMBL493811 IC50 = 9314.0 nM 5.03
CHEMBL495677 IC50 > 10000.0 nM -
CHEMBL497328 IC50 > 10000.0 nM -
CHEMBL497327 IC50 > 10000.0 nM -
CHEMBL493791 IC50 > 10000.0 nM -
CHEMBL524007 IC50 > 10000.0 nM -