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Assay Detail

CHEMBL829697

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

Binding
Inhibition of [125I]NDP-alpha-MSH binding to melanocortin-5 receptor expressed in HEK293 cells
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Melanocortin receptor 5 (CHEMBL4608)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a beta-MSH-derived MC-4R selective agonist.
Mayer JP, Hsiung HM, Flora DB, Edwards P, Smith DP, Zhang XY, Gadski RA, Heiman ML, Hertel JL, Emmerson PJ, Husain S, O'brien TP, Kahl SD, Smiley DL, Zhang L, Dimarchi RD, Yan LZ.
J Med Chem (2005) 48 : 3095 -3098
PubMed 15857110 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 7.98 9.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL415165 1 9.77
CHEMBL414718 1 9.59
CHEMBL266879 1 9.08
CHEMBL428326 1 7.61
CHEMBL412523 1 7.42
CHEMBL415661 1 7.38
CHEMBL427666 1 7.21
CHEMBL412536 1 7.11
CHEMBL407809 1 6.62
CHEMBL267900 1 -
CHEMBL408257 1 -
CHEMBL412495 1 -
CHEMBL412494 1 -
CHEMBL385556 1 -
CHEMBL264132 1 -
CHEMBL2373515 1 -
CHEMBL264352 1 -
CHEMBL410672 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL415165 Ki = 0.17 nM 9.77
CHEMBL414718 Ki = 0.26 nM 9.59
CHEMBL266879 Ki = 0.84 nM 9.08
CHEMBL428326 Ki = 24.8 nM 7.61
CHEMBL412523 Ki = 37.8 nM 7.42
CHEMBL415661 Ki = 42.19 nM 7.38
CHEMBL427666 Ki = 62.11 nM 7.21
CHEMBL412536 Ki = 76.9 nM 7.11
CHEMBL407809 Ki = 239.3 nM 6.62
CHEMBL267900 Ki > 500.0 nM -
CHEMBL408257 Ki > 500.0 nM -
CHEMBL412495 Ki > 500.0 nM -
CHEMBL412494 Ki > 500.0 nM -
CHEMBL385556 Ki > 500.0 nM -
CHEMBL264132 Ki > 500.0 nM -
CHEMBL2373515 Ki > 500.0 nM -
CHEMBL264352 Ki > 500.0 nM -
CHEMBL410672 Ki > 500.0 nM -