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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