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Assay Detail

CHEMBL910339

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

Binding
Binding affinity to human MC3R
19
Total Activities
19
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 3 (CHEMBL4644)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of potent and selective 1,3,4-trisubstituted-2-oxopiperazine based melanocortin-4 receptor agonists.
Tian X, Mishra RK, Switzer AG, Hu XE, Kim N, Mazur AW, Ebetino FH, Wos JA, Crossdoersen D, Pinney BB, Farmer JA, Sheldon RJ.
Bioorg Med Chem Lett (2006) 16 : 4668 -4673
PubMed 16766182 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 6.91 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL379054 1 9.00
CHEMBL212614 1 9.00
CHEMBL385000 1 8.96
CHEMBL215833 1 8.48
CHEMBL384176 1 8.15
CHEMBL214410 1 7.77
CHEMBL384774 1 7.46
CHEMBL378837 1 7.12
CHEMBL215576 1 6.69
CHEMBL211975 1 6.62
CHEMBL215895 1 6.45
CHEMBL213284 1 6.34
CHEMBL213566 1 6.33
CHEMBL212332 1 5.94
CHEMBL211699 1 5.92
CHEMBL202699 1 5.76
CHEMBL214770 1 5.38
CHEMBL212855 1 5.21
CHEMBL387246 1 4.65

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL379054 Ki = 1.0 nM 9.00
CHEMBL212614 Ki = 1.0 nM 9.00
CHEMBL385000 Ki = 1.1 nM 8.96
CHEMBL215833 Ki = 3.3 nM 8.48
CHEMBL384176 Ki = 7.0 nM 8.15
CHEMBL214410 Ki = 17.0 nM 7.77
CHEMBL384774 Ki = 35.0 nM 7.46
CHEMBL378837 Ki = 75.0 nM 7.12
CHEMBL215576 Ki = 206.0 nM 6.69
CHEMBL211975 Ki = 239.0 nM 6.62
CHEMBL215895 Ki = 352.0 nM 6.45
CHEMBL213284 Ki = 461.0 nM 6.34
CHEMBL213566 Ki = 470.0 nM 6.33
CHEMBL212332 Ki = 1143.0 nM 5.94
CHEMBL211699 Ki = 1195.0 nM 5.92
CHEMBL202699 Ki = 1727.0 nM 5.76
CHEMBL214770 Ki = 4122.0 nM 5.38
CHEMBL212855 Ki = 6107.0 nM 5.21
CHEMBL387246 Ki = 22562.0 nM 4.65