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Assay Detail

CHEMBL710465

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

Functional
Decrease in lizard skin reflectivity (metabotropic activity).
17
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

beta-Methylation of the Phe7 and Trp9 melanotropin side chain pharmacophores affects ligand-receptor interactions and prolonged biological activity.
Haskell-Luevano C, Toth K, Boteju L, Job C, Castrucci AM, Hadley ME, Hruby VJ.
J Med Chem (1997) 40 : 2740 -2749
PubMed 9276019 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 17 8.81 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3350298 2 9.70
CHEMBL430239 MELATONAN 1 9.70
CHEMBL2114258 1 9.52
CHEMBL3350299 2 9.30
CHEMBL441738 AFAMELANOTIDE 4.0 1 9.30
CHEMBL2115249 1 9.00
CHEMBL2114259 1 9.00
CHEMBL3350329 2 9.00
CHEMBL214332 INTERMEDINE 2.0 1 9.00
CHEMBL2115248 1 8.48
CHEMBL2115246 1 8.46
CHEMBL2364550 1 8.18
CHEMBL319752 1 7.96
CHEMBL320459 1 7.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL430239 MELATONAN EC50 = 0.2 nM 9.70
CHEMBL3350298 EC50 = 0.2 nM 9.70
CHEMBL2114258 EC50 = 0.3 nM 9.52
CHEMBL3350299 EC50 = 0.5 nM 9.30
CHEMBL441738 AFAMELANOTIDE EC50 = 0.5 nM 9.30
CHEMBL3350329 EC50 = 1.0 nM 9.00
CHEMBL214332 INTERMEDINE EC50 = 1.0 nM 9.00
CHEMBL2114259 EC50 = 1.0 nM 9.00
CHEMBL3350299 EC50 = 1.0 nM 9.00
CHEMBL2115249 EC50 = 1.0 nM 9.00
CHEMBL3350329 EC50 = 1.43 nM 8.85
CHEMBL2115248 EC50 = 3.33 nM 8.48
CHEMBL2115246 EC50 = 3.44 nM 8.46
CHEMBL2364550 EC50 = 6.67 nM 8.18
CHEMBL319752 EC50 = 11.1 nM 7.96
CHEMBL320459 EC50 = 20.0 nM 7.70
CHEMBL3350298 EC50 = 20.0 nM 7.70