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Assay Detail

CHEMBL866558

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Binding
Binding affinity to MC4 receptor
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Synthesis of Tic-D-Phe Psi[CH2-CH2] isostere and its use in the development of melanocortin receptor agonists.
Tian X, Chen X, Gan L, Hayes JC, Switzer AG, Solinsky MG, Ebetino FH, Wos JA, Pinney BB, Farmer JA, Crossdoersen D, Sheldon RJ.
Bioorg Med Chem Lett (2006) 16 : 1721 -1725
PubMed 16376076 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 7.33 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL437132 1 8.30
CHEMBL380120 1 8.00
CHEMBL206033 1 7.89
CHEMBL381357 1 7.62
CHEMBL203252 1 7.43
CHEMBL380437 1 7.12
CHEMBL202699 1 6.98
CHEMBL206018 1 6.67
CHEMBL444883 1 6.67
CHEMBL383256 1 6.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL437132 Ki = 5.0 nM 8.30
CHEMBL380120 Ki = 10.0 nM 8.00
CHEMBL206033 Ki = 13.0 nM 7.89
CHEMBL381357 Ki = 24.0 nM 7.62
CHEMBL203252 Ki = 37.0 nM 7.43
CHEMBL380437 Ki = 76.0 nM 7.12
CHEMBL202699 Ki = 104.0 nM 6.98
CHEMBL206018 Ki = 214.0 nM 6.67
CHEMBL444883 Ki = 214.0 nM 6.67
CHEMBL383256 Ki = 220.0 nM 6.66