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Assay Detail

CHEMBL881790

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

Binding
Inhibitory concentration against human 5-hydroxytryptamine 2C receptor expressed in CHO-K1 cells using [3H]mesulergine
14
Total Activities
13
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 Expert

Target

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

Publication

6-Acylamino-2-aminoquinolines as potent melanin-concentrating hormone 1 receptor antagonists. Identification, structure-activity relationship, and investigation of binding mode.
Ulven T, Frimurer TM, Receveur JM, Little PB, Rist O, Nørregaard PK, Högberg T.
J Med Chem (2005) 48 : 5684 -5697
PubMed 16134937 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 5.58 6.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL187756 1 6.21
CHEMBL373084 1 6.11
CHEMBL195351 1 5.96
CHEMBL193473 1 5.80
CHEMBL196667 1 5.70
CHEMBL194837 2 5.60
CHEMBL196581 1 5.40
CHEMBL194691 1 5.33
CHEMBL196196 1 5.24
CHEMBL197245 1 5.23
CHEMBL194046 1 4.75
CHEMBL198361 1 -
CHEMBL197050 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL187756 IC50 = 610.0 nM 6.21
CHEMBL373084 IC50 = 770.0 nM 6.11
CHEMBL195351 IC50 = 1100.0 nM 5.96
CHEMBL193473 IC50 = 1600.0 nM 5.80
CHEMBL196667 IC50 = 2000.0 nM 5.70
CHEMBL194837 IC50 = 2500.0 nM 5.60
CHEMBL194837 IC50 = 2600.0 nM 5.58
CHEMBL196581 IC50 = 4000.0 nM 5.40
CHEMBL194691 IC50 = 4700.0 nM 5.33
CHEMBL196196 IC50 = 5700.0 nM 5.24
CHEMBL197245 IC50 = 5900.0 nM 5.23
CHEMBL194046 IC50 = 18000.0 nM 4.75
CHEMBL198361 IC50 > 10000.0 nM -
CHEMBL197050 IC50 > 10000.0 nM -