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Assay Detail

CHEMBL714370

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

Binding
In vitro activation of mouse recombinant Melanocortin-4 receptor.
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Melanocortin receptor 4 (CHEMBL3719)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Structure-activity relationships of the melanocortin tetrapeptide Ac-His-DPhe-Arg-Trp-NH(2) at the mouse melanocortin receptors. 1. Modifications at the His position.
Holder JR, Bauzo RM, Xiang Z, Haskell-Luevano C.
J Med Chem (2002) 45 : 2801 -2810
PubMed 12061882 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 21 6.69 10.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL386583 1 10.06
CHEMBL441738 AFAMELANOTIDE 4.0 1 9.68
CHEMBL214332 INTERMEDINE 2.0 1 8.27
CHEMBL264190 1 7.76
CHEMBL405174 1 7.68
CHEMBL327479 1 7.15
CHEMBL330561 1 7.04
CHEMBL317968 1 6.89
CHEMBL431092 1 6.68
CHEMBL94391 1 6.30
CHEMBL432201 1 6.28
CHEMBL96531 1 6.15
CHEMBL317969 1 6.05
CHEMBL330233 1 6.00
CHEMBL320157 1 5.82
CHEMBL329490 1 5.82
CHEMBL329847 1 5.66
CHEMBL96871 1 5.54
CHEMBL94369 1 5.54
CHEMBL432027 1 5.21
CHEMBL275303 1 4.93

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL386583 EC50 = 0.087 nM 10.06
CHEMBL441738 AFAMELANOTIDE EC50 = 0.21 nM 9.68
CHEMBL214332 INTERMEDINE EC50 = 5.37 nM 8.27
CHEMBL264190 EC50 = 17.2 nM 7.76
CHEMBL405174 EC50 = 21.1 nM 7.68
CHEMBL327479 EC50 = 70.6 nM 7.15
CHEMBL330561 EC50 = 91.2 nM 7.04
CHEMBL317968 EC50 = 128.0 nM 6.89
CHEMBL431092 EC50 = 211.0 nM 6.68
CHEMBL94391 EC50 = 506.0 nM 6.30
CHEMBL432201 EC50 = 528.0 nM 6.28
CHEMBL96531 EC50 = 714.0 nM 6.15
CHEMBL317969 EC50 = 887.0 nM 6.05
CHEMBL330233 EC50 = 1000.0 nM 6.00
CHEMBL320157 EC50 = 1500.0 nM 5.82
CHEMBL329490 EC50 = 1500.0 nM 5.82
CHEMBL329847 EC50 = 2170.0 nM 5.66
CHEMBL96871 EC50 = 2900.0 nM 5.54
CHEMBL94369 EC50 = 2900.0 nM 5.54
CHEMBL432027 EC50 = 6200.0 nM 5.21
CHEMBL275303 EC50 = 11700.0 nM 4.93