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Assay Detail

CHEMBL3297283

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Functional
Agonist activity at wild type human melanocortin-4 receptor expressed in HEK293 cells co-transfected with CRE/beta-galactosidase reporter gene assessed as stimulatory response after 6 hrs
ChEMBL ↗
61
Total Activities
61
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Melanocortin receptor 4 (CHEMBL259) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of tetrapeptides from a mixture based positional scanning library that can restore nM full agonist function of the L106P, I69T, I102S, A219V, C271Y, and C271R human melanocortin-4 polymorphic receptors (hMC4Rs).
Haslach EM, Huang H, Dirain M, Debevec G, Geer P, Santos RG, Giulianotti MA, Pinilla C, Appel JR, Doering SR, Walters MA, Houghten RA, Haskell-Luevano C.
J Med Chem (2014) 57 : 4615 -4628
PubMed 24517312 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 61 7.91 9.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3287323 — — 1 9.92
CHEMBL3287329 — — 1 9.72
CHEMBL3287328 — — 1 9.68
CHEMBL3287322 — — 1 9.62
CHEMBL3287324 — — 1 9.59
CHEMBL491870 — — 1 9.55
CHEMBL3287325 — — 1 9.54
CHEMBL3287326 — — 1 9.40
CHEMBL412536 — — 1 9.38
CHEMBL3287327 — — 1 9.35
CHEMBL2103784 COSYNTROPIN 4.0 1 9.19
CHEMBL214332 INTERMEDINE 2.0 1 9.19
CHEMBL264190 — — 1 9.03
CHEMBL3287059 — — 1 8.97
CHEMBL322610 — — 1 8.90
CHEMBL3287069 — — 1 8.72
CHEMBL405174 — — 1 8.66
CHEMBL3287348 — — 1 8.59
CHEMBL3287338 — — 1 8.44
CHEMBL3287334 — — 1 8.37
CHEMBL3287330 — — 1 8.29
CHEMBL3287072 — — 1 8.28
CHEMBL3287060 — — 1 8.21
CHEMBL3287342 — — 1 8.18
CHEMBL3287336 — — 1 8.13
CHEMBL3287344 — — 1 8.02
CHEMBL3287352 — — 1 7.82
CHEMBL3287350 — — 1 7.82
CHEMBL3287066 — — 1 7.82
CHEMBL3287064 — — 1 7.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3287323 — EC50 = 0.12 nM 9.92
CHEMBL3287329 — EC50 = 0.19 nM 9.72
CHEMBL3287328 — EC50 = 0.21 nM 9.68
CHEMBL3287322 — EC50 = 0.24 nM 9.62
CHEMBL3287324 — EC50 = 0.26 nM 9.59
CHEMBL491870 — EC50 = 0.28 nM 9.55
CHEMBL3287325 — EC50 = 0.29 nM 9.54
CHEMBL3287326 — EC50 = 0.4 nM 9.40
CHEMBL412536 — EC50 = 0.42 nM 9.38
CHEMBL3287327 — EC50 = 0.45 nM 9.35
CHEMBL2103784 COSYNTROPIN EC50 = 0.65 nM 9.19
CHEMBL214332 INTERMEDINE EC50 = 0.65 nM 9.19
CHEMBL264190 — EC50 = 0.93 nM 9.03
CHEMBL3287059 — EC50 = 1.06 nM 8.97
CHEMBL322610 — EC50 = 1.25 nM 8.90
CHEMBL3287069 — EC50 = 1.9 nM 8.72
CHEMBL405174 — EC50 = 2.17 nM 8.66
CHEMBL3287348 — EC50 = 2.6 nM 8.59
CHEMBL3287338 — EC50 = 3.6 nM 8.44
CHEMBL3287334 — EC50 = 4.26 nM 8.37
CHEMBL3287330 — EC50 = 5.1 nM 8.29
CHEMBL3287072 — EC50 = 5.3 nM 8.28
CHEMBL3287060 — EC50 = 6.2 nM 8.21
CHEMBL3287342 — EC50 = 6.65 nM 8.18
CHEMBL3287336 — EC50 = 7.42 nM 8.13
CHEMBL3287344 — EC50 = 9.6 nM 8.02
CHEMBL3287350 — EC50 = 15.0 nM 7.82
CHEMBL3287066 — EC50 = 15.0 nM 7.82
CHEMBL3287352 — EC50 = 15.0 nM 7.82
CHEMBL3287064 — EC50 = 17.0 nM 7.77
CHEMBL3287333 — EC50 = 20.0 nM 7.70
CHEMBL3287356 — EC50 = 21.0 nM 7.68
CHEMBL3287354 — EC50 = 22.0 nM 7.66
CHEMBL3287337 — EC50 = 24.0 nM 7.62
CHEMBL3287074 — EC50 = 28.0 nM 7.55
CHEMBL432201 — EC50 = 32.0 nM 7.50
CHEMBL3287347 — EC50 = 40.0 nM 7.40
CHEMBL3287063 — EC50 = 40.0 nM 7.40
CHEMBL3287061 — EC50 = 40.0 nM 7.40
CHEMBL3287065 — EC50 = 46.0 nM 7.34
CHEMBL3287067 — EC50 = 48.0 nM 7.32
CHEMBL3287343 — EC50 = 57.0 nM 7.24
CHEMBL437050 — EC50 = 73.0 nM 7.14
CHEMBL3287068 — EC50 = 76.0 nM 7.12
CHEMBL3287062 — EC50 = 75.0 nM 7.12
CHEMBL3287339 — EC50 = 89.0 nM 7.05
CHEMBL3287357 — EC50 = 110.0 nM 6.96
CHEMBL3287353 — EC50 = 110.0 nM 6.96
CHEMBL3287331 — EC50 = 114.0 nM 6.94
CHEMBL3287345 — EC50 = 120.0 nM 6.92