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Assay Detail

CHEMBL872344

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

Binding
Inhibition of [125I]-NDP MSH binding towards human melanocortin 4 receptor
27
Total Activities
27
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

Privileged structure-based ligands for melanocortin receptors-tetrahydroquinolines, indoles, and aminotetralines.
Fisher MJ, Backer RT, Husain S, Hsiung HM, Mullaney JT, O'Brian TP, Ornstein PL, Rothhaar RR, Zgombick JM, Briner K.
Bioorg Med Chem Lett (2005) 15 : 4459 -4462
PubMed 16112861 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 27 6.29 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2113154 1 7.30
CHEMBL2113149 1 7.16
CHEMBL2113155 1 7.10
CHEMBL2113152 1 6.85
CHEMBL2113148 1 6.82
CHEMBL2113150 1 6.77
CHEMBL2113151 1 6.75
CHEMBL2113141 1 6.72
CHEMBL338594 1 6.66
CHEMBL2113153 1 6.64
CHEMBL2113145 1 6.62
CHEMBL2113140 1 6.55
CHEMBL2113146 1 6.39
CHEMBL2113136 1 6.30
CHEMBL2113147 1 6.28
CHEMBL2113137 1 6.22
CHEMBL2113142 1 6.16
CHEMBL364553 1 6.05
CHEMBL194368 1 6.05
CHEMBL2113138 1 6.02
CHEMBL2113132 1 5.80
CHEMBL2113134 1 5.68
CHEMBL2113139 1 5.60
CHEMBL2113143 1 5.41
CHEMBL2113144 1 5.38
CHEMBL2113135 1 5.32
CHEMBL2113133 1 5.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2113154 Ki = 50.0 nM 7.30
CHEMBL2113149 Ki = 70.0 nM 7.16
CHEMBL2113155 Ki = 80.0 nM 7.10
CHEMBL2113152 Ki = 140.0 nM 6.85
CHEMBL2113148 Ki = 150.0 nM 6.82
CHEMBL2113150 Ki = 170.0 nM 6.77
CHEMBL2113151 Ki = 180.0 nM 6.75
CHEMBL2113141 Ki = 190.0 nM 6.72
CHEMBL338594 Ki = 220.0 nM 6.66
CHEMBL2113153 Ki = 230.0 nM 6.64
CHEMBL2113145 Ki = 240.0 nM 6.62
CHEMBL2113140 Ki = 280.0 nM 6.55
CHEMBL2113146 Ki = 410.0 nM 6.39
CHEMBL2113136 Ki = 500.0 nM 6.30
CHEMBL2113147 Ki = 530.0 nM 6.28
CHEMBL2113137 Ki = 600.0 nM 6.22
CHEMBL2113142 Ki = 700.0 nM 6.16
CHEMBL364553 Ki = 900.0 nM 6.05
CHEMBL194368 Ki = 900.0 nM 6.05
CHEMBL2113138 Ki = 950.0 nM 6.02
CHEMBL2113132 Ki = 1600.0 nM 5.80
CHEMBL2113134 Ki = 2100.0 nM 5.68
CHEMBL2113139 Ki = 2500.0 nM 5.60
CHEMBL2113143 Ki = 3900.0 nM 5.41
CHEMBL2113144 Ki = 4200.0 nM 5.38
CHEMBL2113135 Ki = 4800.0 nM 5.32
CHEMBL2113133 Ki = 7700.0 nM 5.11