Target Validation Information | |||||
---|---|---|---|---|---|
TTD ID | T32247 | ||||
Target Name | Calcitonin receptor (CALCR) | ||||
Type of Target |
Successful |
||||
Drug Potency against Target | Drug Info | Ki = 2569 nM | [1] | ||
CGNLSTCBLGTYTQDFNKFHZYPQTAIGVGAP-amide | Drug Info | IC50 = 79 nM | [1] | ||
CGNLSTCBLGTYTQDF[DKFHO]YPQTAIGVGAP-amide | Drug Info | IC50 = 5.39 nM | [1] | ||
CGNLSTCMLGTYTQDFc[DKFHK]FPQTAIGVGAP-amide | Drug Info | IC50 = 60 nM | [1] | ||
CGNLSTCMLGTYTQDFc[DKFHO]FPQTAIGVGAP-amide | Drug Info | IC50 = 173 nM | [1] | ||
CGNLSTCMLGTYTQDFNKFHTFPQTAIGVGAP-amide | Drug Info | IC50 = 2450 nM | [1] | ||
CGNLSTCMLGTYTQDFNKPHTFPQTAIGVGAP-amide | Drug Info | Ki = 400 nM | [1] | ||
CGNLSTCMLGTYTQDFNPFHTFPQTAIGVGAP-amide | Drug Info | IC50 = 1905 nM | [1] | ||
CSNLSTCVLGKLSQELc[DKLHK]YPRTNTGSGTP-amide | Drug Info | IC50 = 0.18 nM | [1] | ||
CSNLSTCVLGKLSQELc[DKLHO]YPRTNTGSGTP-amide | Drug Info | IC50 = 0.249 nM | [1] | ||
CSNLSTCVLGKLSQELc[DKLQK]YPRTNTGSGTP-amide | Drug Info | IC50 = 0.326 nM | [1] | ||
CSNLSTCVLGKLSQELHKLQTYPRTNTGSGTP-amide | Drug Info | IC50 = 0.377 nM | [1] | ||
CSNLSTCVLGKLSQELNKLHBYPRTNTGSGTP-amide | Drug Info | IC50 = 0.408 nM | [1] | ||
References | |||||
REF 1 | Side-chain lactam-bridge conformational constraints differentiate the activities of salmon and human calcitonins and reveal a new design concept fo... J Med Chem. 2002 Feb 28;45(5):1108-21. | ||||
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