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Assay Detail

CHEMBL5050084

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

Functional
Agonist activity at human OX2R expressed in CHO-K1 cells by FLIPR calcium flux assay
20
Total Activities
18
Compounds Tested
1
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

Discovery of TAK-925 as a Potent, Selective, and Brain-Penetrant Orexin 2 Receptor Agonist.
Fujimoto T, Rikimaru K, Fukuda K, Sugimoto H, Masuda K, Ohyabu N, Banno Y, Tokunaga N, Kawamoto T, Tomata Y, Kumagai Y, Iida M, Nagano Y, Yoneyama-Hirozane M, Shimizu Y, Sasa K, Ishikawa T, Yukitake H, Ito M, Aoyama K, Matsumoto T.
ACS Med Chem Lett (2022) 13 : 457 -462
PubMed 35295087 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 20 6.98 9.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5079059 1 9.74
CHEMBL5089283 1 9.54
CHEMBL5088323 1 7.96
CHEMBL5072262 1 7.57
CHEMBL5082665 3 7.18
CHEMBL5085597 1 6.57
CHEMBL5085916 1 6.48
CHEMBL5084444 1 6.24
CHEMBL5085320 1 6.03
CHEMBL5091377 1 5.60
CHEMBL5092923 1 5.60
CHEMBL5091864 1 5.43
CHEMBL5094264 1 -
CHEMBL4650341 DANAVOREXTON 2.0 1 -
CHEMBL5083834 1 -
CHEMBL5091670 1 -
CHEMBL5074631 1 -
CHEMBL5073349 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5079059 EC50 = 0.18 nM 9.74
CHEMBL5089283 EC50 = 0.29 nM 9.54
CHEMBL5088323 EC50 = 11.0 nM 7.96
CHEMBL5072262 EC50 = 27.0 nM 7.57
CHEMBL5082665 EC50 = 66.0 nM 7.18
CHEMBL5082665 EC50 = 140.0 nM 6.85
CHEMBL5085597 EC50 = 270.0 nM 6.57
CHEMBL5085916 EC50 = 330.0 nM 6.48
CHEMBL5084444 EC50 = 570.0 nM 6.24
CHEMBL5085320 EC50 = 940.0 nM 6.03
CHEMBL5091377 EC50 = 2500.0 nM 5.60
CHEMBL5092923 EC50 = 2500.0 nM 5.60
CHEMBL5091864 EC50 = 3700.0 nM 5.43
CHEMBL5083834 EC50 > 30000.0 nM -
CHEMBL5094264 EC50 > 30000.0 nM -
CHEMBL5082665 EC50 > 30000.0 nM -
CHEMBL4650341 DANAVOREXTON EC50 = 5.5 nM -
CHEMBL5091670 EC50 > 30000.0 nM -
CHEMBL5074631 EC50 > 30000.0 nM -
CHEMBL5073349 EC50 > 30000.0 nM -