Ki Summary

Reaction Details

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Target

Melanocortin receptor 4

Ligand

BDBM50115373

Substrate/Competitor

n/a

Meas. Tech.

ChEMBL_1365574 (CHEMBL3297283)

EC50

1.3±n/a nM

Citation

Haslach, EM; Huang, H; Dirain, M; Debevec, G; Geer, P; Santos, RG; Giulianotti, MA; Pinilla, C; Appel, JR; Doering, SR; Walters, MA; Houghten, RA; Haskell-Luevano, C Identification of tetrapeptides from a mixture based positional scanning library that can restore nM full agonist function of the L106P, I69T, I102S, A219V, C271Y, and C271R human melanocortin-4 polymorphic receptors (hMC4Rs). J Med Chem57:4615-28 (2014) [PubMed] Article

More Info.:

Get all data from this article, Assay Method

Melanocortin receptor 4

Name:

Melanocortin receptor 4

Synonyms:

Type:

Enzyme

Mol. Mass.:

36949.50

Organism:

Homo sapiens (Human)

Description:

P32245

Residue:

332

Sequence:

MVNSTHRGMHTSLHLWNRSSYRLHSNASESLGKGYSDGGCYEQLFVSPEVFVTLGVISLL
ENILVIVAIAKNKNLHSPMYFFICSLAVADMLVSVSNGSETIVITLLNSTDTDAQSFTVN
IDNVIDSVICSSLLASICSLLSIAVDRYFTIFYALQYHNIMTVKRVGIIISCIWAACTVS
GILFIIYSDSSAVIICLITMFFTMLALMASLYVHMFLMARLHIKRIAVLPGTGAIRQGAN
MKGAITLTILIGVFVVCWAPFFLHLIFYISCPQNPYCVCFMSHFNLYLILIMCNSIIDPL
IYALRSQELRKTFKEIICCYPLGGLCDLSSRY

BDBM50115373

n/a

Name

BDBM50115373

Synonyms:

2-[2-[2-Acetylamino-3-(3H-imidazol-4-yl)-propionylamino]-3-(4-iodo-phenyl)-propionylamino]-5-guanidino-pentanoic acid [1-carbamoyl-2-(1H-indol-3-yl)-ethyl]-amide | Ac-His-DPhe(pI)-Arg-Trp-NH2 | CHEMBL322610

Type

Small organic molecule

Emp. Form.

C34H42IN11O5

Mol. Mass.

811.6725

SMILES

CC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccc(I)cc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(N)=O |r,wU:4.3,14.14,26.27,wD:37.38,(23.38,-8.66,;23.38,-10.2,;22.06,-10.96,;24.72,-10.97,;26.05,-10.21,;26.05,-8.66,;27.39,-7.89,;28.79,-8.52,;29.83,-7.38,;29.06,-6.04,;27.55,-6.36,;27.39,-10.97,;27.39,-12.51,;28.72,-10.21,;30.06,-10.97,;30.06,-12.51,;31.39,-13.29,;32.73,-12.51,;34.05,-13.29,;34.05,-14.83,;35.38,-15.6,;32.72,-15.59,;31.39,-14.82,;31.39,-10.21,;31.39,-8.66,;32.72,-10.97,;34.05,-10.2,;34.05,-8.67,;35.38,-7.89,;35.38,-6.36,;36.72,-5.59,;36.72,-4.06,;35.39,-3.28,;38.06,-3.28,;35.38,-10.97,;35.38,-12.52,;36.72,-10.21,;38.06,-10.98,;38.06,-12.52,;39.39,-13.3,;40.8,-12.67,;41.82,-13.82,;41.06,-15.15,;41.52,-16.62,;40.5,-17.76,;38.99,-17.44,;38.51,-15.97,;39.55,-14.83,;39.39,-10.22,;40.73,-10.98,;39.39,-8.68,)|

Structure