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Assay Detail

CHEMBL854881

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

Binding
Inhibition of binding to serotonin receptor 5HT2C
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 2C (CHEMBL225)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel pyrazolopiperazinone- and pyrrolopiperazinone-based MCH-R1 antagonists.
Meyers KM, Méndez-Andino J, Colson AO, Hu XE, Wos JA, Mitchell MC, Hodge K, Howard J, Paris JL, Dowty ME, Obringer CM, Reizes O.
Bioorg Med Chem Lett (2007) 17 : 657 -661
PubMed 17174091 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 6.01 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL216280 1 7.00
CHEMBL216242 1 6.16
CHEMBL450942 1 5.60
CHEMBL217196 1 5.28
CHEMBL408198 1 -
CHEMBL217861 1 -
CHEMBL217140 1 -
CHEMBL385340 1 -
CHEMBL217351 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL216280 Ki = 100.0 nM 7.00
CHEMBL216242 Ki = 700.0 nM 6.16
CHEMBL450942 Ki = 2500.0 nM 5.60
CHEMBL217196 Ki = 5300.0 nM 5.28
CHEMBL408198 Ki > 100000.0 nM -
CHEMBL217861 Ki > 100000.0 nM -
CHEMBL217140 Ki > 100000.0 nM -
CHEMBL385340 Ki > 100000.0 nM -
CHEMBL217351 Ki > 100000.0 nM -