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Assay Detail

CHEMBL857326

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Functional
Agonist selectivity for orexin receptor 1 versus orexin receptor 2
63
Total Activities
61
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Development of an orexin-2 receptor selective agonist, [Ala(11), D-Leu(15)]orexin-B.
Asahi S, Egashira S, Matsuda M, Iwaasa H, Kanatani A, Ohkubo M, Ihara M, Morishima H.
Bioorg Med Chem Lett (2003) 13 : 111 -113
PubMed 12467628 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 60 7.94 8.64
selectivity 3 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL265504 1 8.64
CHEMBL386549 1 8.62
CHEMBL439541 1 8.49
CHEMBL440060 1 8.42
CHEMBL436915 1 8.35
CHEMBL409968 1 8.29
CHEMBL410899 1 8.28
CHEMBL265907 1 8.26
CHEMBL410947 1 8.24
CHEMBL441008 1 8.23
CHEMBL264482 1 8.22
CHEMBL428123 1 8.17
CHEMBL430313 1 8.16
CHEMBL264342 1 8.15
CHEMBL413884 1 8.10
CHEMBL410816 1 8.09
CHEMBL265746 1 8.08
CHEMBL265423 1 8.08
CHEMBL439288 1 8.08
CHEMBL427771 1 8.04
CHEMBL411174 1 8.03
CHEMBL409301 1 8.00
CHEMBL409970 1 8.00
CHEMBL413434 OREXIN B 3 8.00
CHEMBL410960 1 7.96
CHEMBL442505 1 7.96
CHEMBL414332 1 7.96
CHEMBL410898 1 7.96
CHEMBL264343 1 7.92
CHEMBL409456 1 7.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL265504 EC50 = 2.3 nM 8.64
CHEMBL386549 EC50 = 2.4 nM 8.62
CHEMBL439541 EC50 = 3.2 nM 8.49
CHEMBL440060 EC50 = 3.8 nM 8.42
CHEMBL436915 EC50 = 4.5 nM 8.35
CHEMBL409968 EC50 = 5.1 nM 8.29
CHEMBL410899 EC50 = 5.3 nM 8.28
CHEMBL265907 EC50 = 5.5 nM 8.26
CHEMBL410947 EC50 = 5.8 nM 8.24
CHEMBL441008 EC50 = 5.9 nM 8.23
CHEMBL264482 EC50 = 6.0 nM 8.22
CHEMBL428123 EC50 = 6.8 nM 8.17
CHEMBL430313 EC50 = 6.9 nM 8.16
CHEMBL264342 EC50 = 7.1 nM 8.15
CHEMBL413884 EC50 = 7.9 nM 8.10
CHEMBL410816 EC50 = 8.2 nM 8.09
CHEMBL265746 EC50 = 8.3 nM 8.08
CHEMBL439288 EC50 = 8.3 nM 8.08
CHEMBL265423 EC50 = 8.4 nM 8.08
CHEMBL427771 EC50 = 9.2 nM 8.04
CHEMBL411174 EC50 = 9.4 nM 8.03
CHEMBL413434 OREXIN B EC50 = 10.0 nM 8.00
CHEMBL413434 OREXIN B EC50 = 10.0 nM 8.00
CHEMBL409301 EC50 = 10.0 nM 8.00
CHEMBL409970 EC50 = 10.0 nM 8.00
CHEMBL410960 EC50 = 11.0 nM 7.96
CHEMBL414332 EC50 = 11.0 nM 7.96
CHEMBL410898 EC50 = 11.0 nM 7.96
CHEMBL442505 EC50 = 11.0 nM 7.96
CHEMBL264343 EC50 = 12.0 nM 7.92
CHEMBL409456 EC50 = 12.0 nM 7.92
CHEMBL414312 EC50 = 12.0 nM 7.92
CHEMBL430064 EC50 = 12.0 nM 7.92
CHEMBL437464 EC50 = 13.0 nM 7.89
CHEMBL413504 EC50 = 13.0 nM 7.89
CHEMBL265404 EC50 = 13.0 nM 7.89
CHEMBL263628 EC50 = 13.0 nM 7.89
CHEMBL413284 EC50 = 13.0 nM 7.89
CHEMBL413285 EC50 = 14.0 nM 7.85
CHEMBL437274 EC50 = 14.0 nM 7.85
CHEMBL410480 EC50 = 14.0 nM 7.85
CHEMBL409676 EC50 = 14.0 nM 7.85
CHEMBL430080 EC50 = 15.0 nM 7.82
CHEMBL266409 EC50 = 15.0 nM 7.82
CHEMBL438036 EC50 = 16.0 nM 7.80
CHEMBL269780 EC50 = 16.0 nM 7.80
CHEMBL411116 EC50 = 17.0 nM 7.77
CHEMBL442503 EC50 = 18.0 nM 7.75
CHEMBL409967 EC50 = 26.0 nM 7.58
CHEMBL275985 EC50 = 28.0 nM 7.55