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Assay Detail

CHEMBL662310

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

Functional
Functional potency was determined by concentration required for activation of OX1 (Orexin-1) receptor expressed in chinese hamster ovary cells (CHO) and increasing the intracellular calcium concentration
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cricetulus griseus
Cell Type ovary
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

ADMET (CHEMBL612558)
Type ADMET

Publication

Structure-activity analysis of truncated orexin-A analogues at the orexin-1 receptor.
Darker JG, Porter RA, Eggleston DS, Smart D, Brough SJ, Sabido-David C, Jerman JC.
Bioorg Med Chem Lett (2001) 11 : 737 -740
PubMed 11266181 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 9 6.51 8.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL438925 1 8.68
CHEMBL437062 1 6.71
CHEMBL413221 1 6.46
CHEMBL412459 1 6.45
CHEMBL414285 1 6.19
CHEMBL268561 1 6.11
CHEMBL438753 1 6.08
CHEMBL414043 1 6.00
CHEMBL267753 1 5.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL438925 EC50 = 2.089 nM 8.68
CHEMBL437062 EC50 = 194.98 nM 6.71
CHEMBL413221 EC50 = 346.74 nM 6.46
CHEMBL412459 EC50 = 354.81 nM 6.45
CHEMBL414285 EC50 = 645.65 nM 6.19
CHEMBL268561 EC50 = 776.25 nM 6.11
CHEMBL438753 EC50 = 831.76 nM 6.08
CHEMBL414043 EC50 = 1000.0 nM 6.00
CHEMBL267753 EC50 = 1288.25 nM 5.89