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Assay Detail

CHEMBL3579242

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

Binding
Displacement of MTII from mouse MC4R expressed in HEK293 cells
ChEMBL ↗
49
Total Activities
29
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery of a β-Hairpin Octapeptide, c[Pro-Arg-Phe-Phe-Dap-Ala-Phe-DPro], Mimetic of Agouti-Related Protein(87-132) [AGRP(87-132)] with Equipotent Mouse Melanocortin-4 Receptor (mMC4R) Antagonist Pharmacology.
Ericson MD, Wilczynski A, Sorensen NB, Xiang Z, Haskell-Luevano C.
J Med Chem (2015) 58 : 4638 -4647
PubMed 25898270 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 28 7.62 10.40
Ki 20 7.52 9.10
IC50 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3422426 — — 1 10.40
CHEMBL3577996 — — 2 9.10
CHEMBL3577997 — — 2 8.40
CHEMBL3577995 — — 2 8.40
CHEMBL3578000 — — 2 8.40
CHEMBL3577998 — — 2 8.30
CHEMBL3577999 — — 2 8.30
CHEMBL3577991 — — 2 8.20
CHEMBL3577993 — — 2 7.80
CHEMBL3577986 — — 2 7.80
CHEMBL3577981 — — 2 7.70
CHEMBL3577978 — — 2 7.20
CHEMBL3577994 — — 2 7.20
CHEMBL3577985 — — 2 7.00
CHEMBL3577987 — — 2 7.00
CHEMBL3577988 — — 2 6.80
CHEMBL3578001 — — 1 6.80
CHEMBL3577982 — — 2 6.80
CHEMBL3577980 — — 1 6.80
CHEMBL3577979 — — 2 6.80
CHEMBL3577977 — — 2 6.80
CHEMBL3577976 — — 2 6.50
CHEMBL3577990 — — 2 5.90
CHEMBL3578004 — — 1 -
CHEMBL3577992 — — 1 -
CHEMBL3577989 — — 1 -
CHEMBL3576882 — — 1 -
CHEMBL3577984 — — 1 -
CHEMBL3577983 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3422426 — Kd = 0.03981 nM 10.40
CHEMBL3577996 — Ki = 0.79 nM 9.10
CHEMBL3577996 — Kd = 0.7943 nM 9.10
CHEMBL3578000 — Ki = 4.0 nM 8.40
CHEMBL3577997 — Ki = 4.0 nM 8.40
CHEMBL3577995 — Ki = 4.0 nM 8.40
CHEMBL3578000 — Kd = 3.981 nM 8.40
CHEMBL3577997 — Kd = 3.981 nM 8.40
CHEMBL3577995 — Kd = 3.981 nM 8.40
CHEMBL3577998 — Ki = 5.0 nM 8.30
CHEMBL3577998 — Kd = 5.012 nM 8.30
CHEMBL3577999 — Ki = 5.0 nM 8.30
CHEMBL3577999 — Kd = 5.012 nM 8.30
CHEMBL3577991 — Kd = 6.31 nM 8.20
CHEMBL3577991 — Ki = 6.3 nM 8.20
CHEMBL3577993 — Kd = 15.85 nM 7.80
CHEMBL3577986 — Kd = 15.85 nM 7.80
CHEMBL3577986 — Ki = 16.0 nM 7.80
CHEMBL3577993 — Ki = 16.0 nM 7.80
CHEMBL3577981 — Ki = 20.0 nM 7.70
CHEMBL3577981 — Kd = 19.95 nM 7.70
CHEMBL3577994 — Ki = 63.0 nM 7.20
CHEMBL3577978 — Ki = 63.0 nM 7.20
CHEMBL3577978 — Kd = 63.1 nM 7.20
CHEMBL3577994 — Kd = 63.1 nM 7.20
CHEMBL3577985 — Kd = 100.0 nM 7.00
CHEMBL3577985 — Ki = 100.0 nM 7.00
CHEMBL3577987 — Ki = 100.0 nM 7.00
CHEMBL3577987 — Kd = 100.0 nM 7.00
CHEMBL3577977 — Ki = 160.0 nM 6.80
CHEMBL3578001 — Kd = 158.49 nM 6.80
CHEMBL3577979 — Ki = 160.0 nM 6.80
CHEMBL3577982 — Ki = 160.0 nM 6.80
CHEMBL3577988 — Kd = 158.49 nM 6.80
CHEMBL3577980 — Kd = 158.49 nM 6.80
CHEMBL3577977 — Kd = 158.49 nM 6.80
CHEMBL3577982 — Kd = 158.49 nM 6.80
CHEMBL3577988 — Ki = 160.0 nM 6.80
CHEMBL3577976 — Ki = 320.0 nM 6.50
CHEMBL3577976 — Kd = 316.23 nM 6.50
CHEMBL3577990 — Kd = 1258.93 nM 5.90
CHEMBL3577990 — Ki = 1300.0 nM 5.89
CHEMBL3578004 — IC50 - — -
CHEMBL3577983 — Kd > 100000.0 nM -
CHEMBL3577984 — Kd > 100000.0 nM -
CHEMBL3576882 — Kd > 100000.0 nM -
CHEMBL3577992 — Kd > 100000.0 nM -
CHEMBL3577979 — Kd > 100000.0 nM -
CHEMBL3577989 — Kd > 100000.0 nM -