Target Validation Information
TTD ID	T26851
Target Name	Complement C3 (CO3)
Type of Target	Successful
Drug Potency against Target		Drug Info	IC50 = 1400 nM	[1]
		Drug Info	IC50 = 870 nM	[2]
		Drug Info	IC50 = 3000 nM	[1]
	Ac-ICV(5fW)QDWGAHRCT-NH2	Drug Info	IC50 = 1740 nM	[2]
	Ac-ICVWQD(5fW)GAHRCT-NH2	Drug Info	IC50 = 446 nM	[2]
	Ac-ICVWQDWGAHRCT-NH2	Drug Info	IC50 = 1200 nM	[2]
	Ac-I[CV(1Nal)QDWGAHRC]T	Drug Info	IC50 = 1800 nM	[1]
	Ac-I[CV(2Igl)QDWGAHRC]T	Drug Info	IC50 = 1500 nM	[1]
	Ac-I[CV(2Nal)QDWGAHRC]T	Drug Info	IC50 = 1400 nM	[1]
	Ac-I[CV(2Nal)QDWGAHRC]T-NH2	Drug Info	IC50 = 500 nM	[1]
	Ac-I[CV(Bpa)QDWGAHRC]T	Drug Info	IC50 = 1100 nM	[1]
	Ac-I[CV(Bpa)QDWGAHRC]T-NH2	Drug Info	IC50 = 600 nM	[1]
	Ac-I[CV(Bta)QDWGAHRC]T	Drug Info	IC50 = 800 nM	[1]
	Ac-I[CV(Bta)QDWGAHRC]T-NH2	Drug Info	IC50 = 800 nM	[1]
	Ac-I[CV(Dht)QDWGAHRC]T	Drug Info	IC50 = 10200 nM	[1]
	Ac-I[CV(Yphs)QDWGAHRC]I-NH2	Drug Info	IC50 = 9600 nM	[1]
	Ac-I[CVFQDWGHHRC]T-NH2	Drug Info	IC50 = 6000 nM	[1]
	Ac-I[CVHQDWGHHRC]T-NH2	Drug Info	IC50 = 7000 nM	[1]
	Ac-I[CVSQDWGHHRC]T-NH2	Drug Info	IC50 = 6000 nM	[1]
	Ac-I[CVTQDWGHHRC]T-NH2	Drug Info	IC50 = 6000 nM	[1]
	Ac-I[CVVQDWGAHRC]T-NH2	Drug Info	IC50 = 13000 nM	[1]
	Ac-I[CVWQDWG(Abu)HRC]T-NH2	Drug Info	IC50 = 1500 nM	[1]
	Ac-I[CVWQDWGAHRC]dT	Drug Info	IC50 = 2700 nM	[1]
	Ac-I[CVWQDWGAHRC]T	Drug Info	IC50 = 12000 nM	[1]
	Ac-I[CVWQDWGHHRC]T-NH2	Drug Info	IC50 = 7000 nM	[1]
	Ac-I[CVWQDWGWHRC]T-NH2	Drug Info	IC50 = 6000 nM	[1]
References
REF 1	Design and NMR characterization of active analogues of compstatin containing non-natural amino acids. J Med Chem. 2005 Jan 13;48(1):274-86.
REF 2	Hydrophobic effect and hydrogen bonds account for the improved activity of a complement inhibitor, compstatin. J Med Chem. 2006 Jul 27;49(15):4616-22.

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