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Assay Detail

CHEMBL3579241

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

Binding
Displacement of MTII from mouse MC3R expressed in HEK293 cells
ChEMBL ↗
46
Total Activities
31
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 3 (CHEMBL4774) ↗
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 30 6.58 9.50
Ki 15 6.45 7.60
IC50 1 6.90 6.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3422426 — — 1 9.50
CHEMBL3577995 — — 2 7.60
CHEMBL3577999 — — 2 7.00
CHEMBL3577997 — — 2 7.00
CHEMBL3578004 — — 1 6.90
CHEMBL3577996 — — 2 6.90
CHEMBL3577998 — — 2 6.80
CHEMBL3578000 — — 2 6.70
CHEMBL3577981 — — 2 6.40
CHEMBL3577978 — — 2 6.20
CHEMBL3578003 — — 1 6.20
CHEMBL3577977 — — 2 6.20
CHEMBL3577982 — — 2 6.20
CHEMBL3577976 — — 2 6.10
CHEMBL3578002 — — 1 6.10
CHEMBL3577986 — — 2 6.10
CHEMBL3577987 — — 2 6.00
CHEMBL3577980 — — 1 5.90
CHEMBL3577979 — — 2 5.89
CHEMBL3577993 — — 2 5.60
CHEMBL3577994 — — 1 -
CHEMBL3576882 — — 1 -
CHEMBL3577985 — — 1 -
CHEMBL3577984 — — 1 -
CHEMBL3577983 — — 1 -
CHEMBL3577992 — — 1 -
CHEMBL3578001 — — 1 -
CHEMBL3577991 — — 1 -
CHEMBL3577990 — — 1 -
CHEMBL3577989 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3422426 — Kd = 0.3162 nM 9.50
CHEMBL3577995 — Ki = 25.0 nM 7.60
CHEMBL3577995 — Kd = 25.12 nM 7.60
CHEMBL3577999 — Ki = 100.0 nM 7.00
CHEMBL3577997 — Ki = 100.0 nM 7.00
CHEMBL3577999 — Kd = 100.0 nM 7.00
CHEMBL3577997 — Kd = 100.0 nM 7.00
CHEMBL3578004 — IC50 = 127.0 nM 6.90
CHEMBL3577996 — Kd = 125.89 nM 6.90
CHEMBL3577996 — Ki = 130.0 nM 6.89
CHEMBL3577998 — Ki = 160.0 nM 6.80
CHEMBL3577998 — Kd = 158.49 nM 6.80
CHEMBL3578000 — Kd = 199.53 nM 6.70
CHEMBL3578000 — Ki = 200.0 nM 6.70
CHEMBL3577981 — Ki = 400.0 nM 6.40
CHEMBL3577981 — Kd = 398.11 nM 6.40
CHEMBL3577978 — Kd = 630.96 nM 6.20
CHEMBL3577977 — Kd = 630.96 nM 6.20
CHEMBL3577978 — Ki = 630.0 nM 6.20
CHEMBL3577977 — Ki = 630.0 nM 6.20
CHEMBL3577982 — Kd = 630.96 nM 6.20
CHEMBL3578003 — Kd = 630.96 nM 6.20
CHEMBL3577982 — Ki = 630.0 nM 6.20
CHEMBL3577976 — Kd = 794.33 nM 6.10
CHEMBL3578002 — Kd = 794.33 nM 6.10
CHEMBL3577986 — Ki = 790.0 nM 6.10
CHEMBL3577976 — Ki = 790.0 nM 6.10
CHEMBL3577986 — Kd = 794.33 nM 6.10
CHEMBL3577987 — Ki = 1000.0 nM 6.00
CHEMBL3577987 — Kd = 1000.0 nM 6.00
CHEMBL3577980 — Kd = 1258.93 nM 5.90
CHEMBL3577979 — Ki = 1300.0 nM 5.89
CHEMBL3577993 — Ki = 2500.0 nM 5.60
CHEMBL3577993 — Kd = 2511.89 nM 5.60
CHEMBL3577990 — Kd > 100000.0 nM -
CHEMBL3577991 — Kd > 100000.0 nM -
CHEMBL3577992 — Kd > 100000.0 nM -
CHEMBL3577994 — Kd > 100000.0 nM -
CHEMBL3577988 — Kd > 100000.0 nM -
CHEMBL3576882 — Kd > 100000.0 nM -
CHEMBL3577985 — Kd > 100000.0 nM -
CHEMBL3577984 — Kd > 100000.0 nM -
CHEMBL3578001 — Kd > 100000.0 nM -
CHEMBL3577983 — Kd > 100000.0 nM -
CHEMBL3577989 — Kd > 100000.0 nM -
CHEMBL3577979 — Kd > 100000.0 nM -