Ki Summary

Reaction Details

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Target

Melanocortin receptor 5

Ligand

BDBM50268803

Substrate/Competitor

n/a

Meas. Tech.

ChEMBL_523579 (CHEMBL997229)

EC50

<0.1±n/a nM

Comments

Zero 20220115

Citation

Qu, H; Cai, M; Mayorov, AV; Grieco, P; Zingsheim, M; Trivedi, D; Hruby, VJ Substitution of arginine with proline and proline derivatives in melanocyte-stimulating hormones leads to selectivity for human melanocortin 4 receptor. J Med Chem52:3627-35 (2009) [PubMed] Article

More Info.:

Get all data from this article, Assay Method

Melanocortin receptor 5

Name:

Melanocortin receptor 5

Synonyms:

Type:

Enzyme

Mol. Mass.:

36612.92

Organism:

Homo sapiens (Human)

Description:

P33032

Residue:

325

Sequence:

MNSSFHLHFLDLNLNATEGNLSGPNVKNKSSPCEDMGIAVEVFLTLGVISLLENILVIGA
IVKNKNLHSPMYFFVCSLAVADMLVSMSSAWETITIYLLNNKHLVIADAFVRHIDNVFDS
MICISVVASMCSLLAIAVDRYVTIFYALRYHHIMTARRSGAIIAGIWAFCTGCGIVFILY
SESTYVILCLISMFFAMLFLLVSLYIHMFLLARTHVKRIAALPGASSARQRTSMQGAVTV
TMLLGVFTVCWAPFFLHLTLMLSCPQNLYCSRFMSHFNMYLILIMCNSVMDPLIYAFRSQ
EMRKTFKEIICCRGFRIACSFPRRD

BDBM50268803

n/a

Name

BDBM50268803

Synonyms:

Ac-Tyr-Val-Nle-Gly-His-DPhe-cis-Xaa-Trp-Asp-Arg-Phe-Gly-NH2 | CHEMBL525399

Type

Small organic molecule

Emp. Form.

C77H102N22O16

Mol. Mass.

1591.7716

SMILES

CCCC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(C)=O)C(C)C)C(=O)NCC(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](Cc1ccccc1)C(=O)N1C[C@H](C[C@H]1C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1ccccc1)C(=O)NCC(N)=O)N=C(N)N |r,wU:8.8,45.46,59.63,57.117,96.101,35.35,77.82,wD:4.4,12.21,63.66,85.90,(2.53,-50.05,;1.21,-50.83,;-.13,-50.07,;-1.45,-50.85,;-2.8,-50.09,;-4.13,-50.88,;-4.11,-52.42,;-2.77,-53.17,;-5.44,-53.2,;-5.43,-54.75,;-6.75,-55.53,;-8.09,-54.77,;-6.74,-57.06,;-5.4,-57.82,;-4.07,-57.04,;-4.09,-55.5,;-2.76,-54.71,;-1.41,-55.47,;-.08,-54.68,;-1.39,-57.02,;-2.73,-57.8,;-8.07,-57.85,;-8.06,-59.39,;-9.38,-60.18,;-6.71,-60.14,;-6.78,-52.45,;-6.8,-50.91,;-8.1,-53.23,;-2.82,-48.56,;-4.16,-47.8,;-1.49,-47.77,;-1.51,-46.23,;-.18,-45.44,;1.17,-46.2,;-.2,-43.9,;1.13,-43.12,;1.11,-41.58,;-.23,-40.83,;-.4,-39.3,;-1.91,-38.99,;-2.66,-40.33,;-1.63,-41.47,;2.47,-43.88,;2.49,-45.42,;3.8,-43.1,;5.14,-43.85,;5.16,-45.4,;6.5,-46.15,;6.51,-47.7,;7.85,-48.46,;9.17,-47.68,;9.16,-46.14,;7.81,-45.37,;6.5,-43.14,;7.76,-44.04,;6.57,-41.61,;5.55,-40.45,;6.33,-39.12,;7.84,-39.46,;7.99,-40.99,;9.31,-41.78,;9.3,-43.32,;10.65,-41.02,;11.97,-41.82,;11.95,-43.36,;13.23,-44.22,;14.68,-43.68,;15.63,-44.89,;14.78,-46.18,;15.16,-47.67,;14.06,-48.75,;12.58,-48.33,;12.19,-46.84,;13.3,-45.76,;13.31,-41.06,;13.32,-39.52,;14.64,-41.85,;15.98,-41.1,;15.99,-39.56,;17.33,-38.8,;18.67,-39.57,;17.35,-37.26,;17.3,-41.87,;17.29,-43.42,;18.65,-41.12,;19.96,-41.91,;19.94,-43.46,;21.27,-44.24,;21.26,-45.78,;22.59,-46.55,;22.56,-48.09,;21.24,-48.84,;23.9,-48.86,;21.3,-41.16,;21.31,-39.62,;22.64,-41.93,;23.98,-41.17,;23.99,-39.64,;25.33,-38.88,;26.66,-39.66,;28.01,-38.91,;28.02,-37.37,;26.7,-36.58,;25.36,-37.34,;25.31,-41.95,;25.29,-43.5,;26.65,-41.2,;27.97,-41.99,;29.31,-41.23,;30.64,-42.01,;29.32,-39.69,;5.72,-37.71,;6.64,-36.47,;6.03,-35.06,;8.17,-36.65,)|

Structure