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Assay Detail

CHEMBL5385068

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Functional
Agonist activity at human OX2R expressed in CHO-K1 cells assessed as increase in intracellular calcium
20
Total Activities
20
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Orexin receptor type 2 (CHEMBL4792)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and Synthesis of Orexin 1 Receptor-Selective Agonists.
Iio K, Hashimoto K, Nagumo Y, Amezawa M, Hasegawa T, Yamamoto N, Kutsumura N, Takeuchi K, Ishikawa Y, Yamamoto H, Tokuda A, Sato T, Uchida Y, Inoue A, Tanimura R, Yanagisawa M, Nagase H, Saitoh T.
J Med Chem (2023) 66 : 5453 -5464
PubMed 37043436 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 19 6.02 6.84
Activity 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5434113 1 6.84
CHEMBL5417451 1 6.78
CHEMBL5423828 1 6.72
CHEMBL5396114 1 6.64
CHEMBL5410801 1 6.56
CHEMBL5415350 1 6.53
CHEMBL5407752 1 6.02
CHEMBL5422867 1 5.99
CHEMBL5411141 1 5.89
CHEMBL5393867 1 5.78
CHEMBL5406322 1 5.62
CHEMBL5422351 1 5.48
CHEMBL5410302 1 5.19
CHEMBL5403398 1 5.15
CHEMBL5394185 1 5.07
CHEMBL5438232 1 -
CHEMBL5403259 1 -
CHEMBL5405864 1 -
CHEMBL5428873 1 -
CHEMBL5406525 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5434113 EC50 = 146.0 nM 6.84
CHEMBL5417451 EC50 = 168.0 nM 6.78
CHEMBL5423828 EC50 = 192.0 nM 6.72
CHEMBL5396114 EC50 = 229.0 nM 6.64
CHEMBL5410801 EC50 = 275.0 nM 6.56
CHEMBL5415350 EC50 = 295.0 nM 6.53
CHEMBL5407752 EC50 = 955.0 nM 6.02
CHEMBL5422867 EC50 = 1015.0 nM 5.99
CHEMBL5411141 EC50 = 1289.0 nM 5.89
CHEMBL5393867 EC50 = 1661.0 nM 5.78
CHEMBL5406322 EC50 = 2411.0 nM 5.62
CHEMBL5422351 EC50 = 3290.0 nM 5.48
CHEMBL5410302 EC50 = 6410.0 nM 5.19
CHEMBL5403398 EC50 = 7010.0 nM 5.15
CHEMBL5394185 EC50 = 8551.0 nM 5.07
CHEMBL5438232 EC50 > 10000.0 nM -
CHEMBL5403259 EC50 > 10000.0 nM -
CHEMBL5405864 EC50 > 10000.0 nM -
CHEMBL5428873 EC50 > 10000.0 nM -
CHEMBL5406525 Activity - -