| Target Validation Information | |||||
|---|---|---|---|---|---|
| Target ID | T36098 | ||||
| Target Name | Farnesyl pyrophosphatesynthetase | ||||
| Target Type | Successful |
||||
| Drug Potency against Target | Risedronate | Drug Info | IC50 = 3.9 nM | [552653] | |
| Ibandronate | Drug Info | IC50 = 20 nM/L | [552653] | ||
| NERIDRONIC ACID | Drug Info | Ki = 63.5 nM | [529362] | ||
| NE-10575 | Drug Info | Ki = 3.9 nM | [529362] | ||
| Piridronic acid | Drug Info | Ki = 4.45 nM | [529362] | ||
| [2-(Imidazol-1-yl)ethyl]-bisphosphonic acid | Drug Info | IC50 = 9.03 nM | [529758] | ||
| Alendronate | Drug Info | IC50 = 50 nMol/L | [552653] | ||
| [2-(6-Chloro-purin-9-yl)ethyl]-bisphosphonic acid | Drug Info | IC50 = 883.1 nM | [529758] | ||
| (biphenyl-3-ylamino)methylenediphosphonic acid | Drug Info | IC50 = 8500 nM | [529690] | ||
| 1-(but-2-ylamino)ethyl 1,I-bisphosphonic acid | Drug Info | IC50 = 112 nM | [529229] | ||
| [2-(Imidazol-2-yl-thio)ethyl]-bisphosphonic acid | Drug Info | IC50 = 28.1 nM | [529758] | ||
| 1-[(n-but-1-ylamino)ethyl]-1,1-bisphosphonic acid | Drug Info | IC50 = 2280 nM | [529229] | ||
| Incadronate | Drug Info | Ki = 10 nM | [529362] | ||
| [2-(Benzoimidazol-1-yl)ethyl]-bisphosphonic acid | Drug Info | IC50 = 16.1 nM | [529758] | ||
| 1-[(cyclohexylamino)ethyl]-1,1-bisphosphonicacid | Drug Info | IC50 = 337 nM | [529229] | ||
| 1-[(n-hex-1-ylamino)ethyl]-1,1-bisphosphonic acid | Drug Info | IC50 = 137 nM | [529229] | ||
| 1-[(prop-1-ylamino)ethyl]-1,1-bisphosphonic acid | Drug Info | IC50 = 298 nM | [529229] | ||
| (1-hydroxy-1-phosphono-heptyl)-phosphonic acid | Drug Info | Ki = 400 nM | [529229] | ||
| [2-(Pyrazol-1-yl)ethyl]-bisphosphonic acid | Drug Info | IC50 = 3069 nM | [529758] | ||
| [2-(Purin-9-yl)ethyl]-bisphosphonic acid | Drug Info | IC50 = 388.2 nM | [529758] | ||
| 1-[(n-oct-1-ylamino)ethyl]-1,1-bisphosphonic acid | Drug Info | IC50 = 87 nM | [529229] | ||
| 1-[(tert-butylamino)ethyl]-1,1-bisphosphonicacid | Drug Info | IC50 = 286 nM | [529229] | ||
| 1-[(prop-2-ylamino)ethyl]-1,1-bisphosphonicacid | Drug Info | IC50 = 253 nM | [529229] | ||
| Pamidronate | Drug Info | IC50 = 200 nMol | [552653] | ||
| References | |||||
| Ref 552653 | Molecular mechanisms of action of bisphosphonates: current status. Clin Cancer Res. 2006 Oct 15;12(20 Pt 2):6222s-6230s. | ||||
| Ref 552653 | Molecular mechanisms of action of bisphosphonates: current status. Clin Cancer Res. 2006 Oct 15;12(20 Pt 2):6222s-6230s. | ||||
| Ref 529362 | J Med Chem. 2008 Apr 10;51(7):2187-95. Epub 2008 Mar 8.Structure-activity relationships among the nitrogen containing bisphosphonates in clinical use and other analogues: time-dependent inhibition of human farnesyl pyrophosphate synthase. | ||||
| Ref 529362 | J Med Chem. 2008 Apr 10;51(7):2187-95. Epub 2008 Mar 8.Structure-activity relationships among the nitrogen containing bisphosphonates in clinical use and other analogues: time-dependent inhibition of human farnesyl pyrophosphate synthase. | ||||
| Ref 529362 | J Med Chem. 2008 Apr 10;51(7):2187-95. Epub 2008 Mar 8.Structure-activity relationships among the nitrogen containing bisphosphonates in clinical use and other analogues: time-dependent inhibition of human farnesyl pyrophosphate synthase. | ||||
| Ref 529758 | J Med Chem. 2008 Nov 13;51(21):6800-7. Epub 2008 Oct 21.Design, synthesis, and biological evaluation of novel aminobisphosphonates possessing an in vivo antitumor activity through a gammadelta-T lymphocytes-mediated activation mechanism. | ||||
| Ref 552653 | Molecular mechanisms of action of bisphosphonates: current status. Clin Cancer Res. 2006 Oct 15;12(20 Pt 2):6222s-6230s. | ||||
| Ref 529758 | J Med Chem. 2008 Nov 13;51(21):6800-7. Epub 2008 Oct 21.Design, synthesis, and biological evaluation of novel aminobisphosphonates possessing an in vivo antitumor activity through a gammadelta-T lymphocytes-mediated activation mechanism. | ||||
| Ref 529690 | Bioorg Med Chem. 2008 Oct 1;16(19):8959-67. Epub 2008 Aug 27.Bisphosphonate inhibitors of ATP-mediated HIV-1 reverse transcriptase catalyzed excision of chain-terminating 3'-azido, 3'-deoxythymidine: a QSAR investigation. | ||||
| Ref 529229 | Bioorg Med Chem. 2008 Mar 15;16(6):3283-90. Epub 2007 Dec 10.Synthesis and biological evaluation of 2-alkylaminoethyl-1,1-bisphosphonic acids against Trypanosoma cruzi and Toxoplasma gondii targeting farnesyl diphosphate synthase. | ||||
| Ref 529758 | J Med Chem. 2008 Nov 13;51(21):6800-7. Epub 2008 Oct 21.Design, synthesis, and biological evaluation of novel aminobisphosphonates possessing an in vivo antitumor activity through a gammadelta-T lymphocytes-mediated activation mechanism. | ||||
| Ref 529229 | Bioorg Med Chem. 2008 Mar 15;16(6):3283-90. Epub 2007 Dec 10.Synthesis and biological evaluation of 2-alkylaminoethyl-1,1-bisphosphonic acids against Trypanosoma cruzi and Toxoplasma gondii targeting farnesyl diphosphate synthase. | ||||
| Ref 529362 | J Med Chem. 2008 Apr 10;51(7):2187-95. Epub 2008 Mar 8.Structure-activity relationships among the nitrogen containing bisphosphonates in clinical use and other analogues: time-dependent inhibition of human farnesyl pyrophosphate synthase. | ||||
| Ref 529758 | J Med Chem. 2008 Nov 13;51(21):6800-7. Epub 2008 Oct 21.Design, synthesis, and biological evaluation of novel aminobisphosphonates possessing an in vivo antitumor activity through a gammadelta-T lymphocytes-mediated activation mechanism. | ||||
| Ref 529229 | Bioorg Med Chem. 2008 Mar 15;16(6):3283-90. Epub 2007 Dec 10.Synthesis and biological evaluation of 2-alkylaminoethyl-1,1-bisphosphonic acids against Trypanosoma cruzi and Toxoplasma gondii targeting farnesyl diphosphate synthase. | ||||
| Ref 529229 | Bioorg Med Chem. 2008 Mar 15;16(6):3283-90. Epub 2007 Dec 10.Synthesis and biological evaluation of 2-alkylaminoethyl-1,1-bisphosphonic acids against Trypanosoma cruzi and Toxoplasma gondii targeting farnesyl diphosphate synthase. | ||||
| Ref 529229 | Bioorg Med Chem. 2008 Mar 15;16(6):3283-90. Epub 2007 Dec 10.Synthesis and biological evaluation of 2-alkylaminoethyl-1,1-bisphosphonic acids against Trypanosoma cruzi and Toxoplasma gondii targeting farnesyl diphosphate synthase. | ||||
| Ref 529229 | Bioorg Med Chem. 2008 Mar 15;16(6):3283-90. Epub 2007 Dec 10.Synthesis and biological evaluation of 2-alkylaminoethyl-1,1-bisphosphonic acids against Trypanosoma cruzi and Toxoplasma gondii targeting farnesyl diphosphate synthase. | ||||
| Ref 529758 | J Med Chem. 2008 Nov 13;51(21):6800-7. Epub 2008 Oct 21.Design, synthesis, and biological evaluation of novel aminobisphosphonates possessing an in vivo antitumor activity through a gammadelta-T lymphocytes-mediated activation mechanism. | ||||
| Ref 529758 | J Med Chem. 2008 Nov 13;51(21):6800-7. Epub 2008 Oct 21.Design, synthesis, and biological evaluation of novel aminobisphosphonates possessing an in vivo antitumor activity through a gammadelta-T lymphocytes-mediated activation mechanism. | ||||
| Ref 529229 | Bioorg Med Chem. 2008 Mar 15;16(6):3283-90. Epub 2007 Dec 10.Synthesis and biological evaluation of 2-alkylaminoethyl-1,1-bisphosphonic acids against Trypanosoma cruzi and Toxoplasma gondii targeting farnesyl diphosphate synthase. | ||||
| Ref 529229 | Bioorg Med Chem. 2008 Mar 15;16(6):3283-90. Epub 2007 Dec 10.Synthesis and biological evaluation of 2-alkylaminoethyl-1,1-bisphosphonic acids against Trypanosoma cruzi and Toxoplasma gondii targeting farnesyl diphosphate synthase. | ||||
| Ref 529229 | Bioorg Med Chem. 2008 Mar 15;16(6):3283-90. Epub 2007 Dec 10.Synthesis and biological evaluation of 2-alkylaminoethyl-1,1-bisphosphonic acids against Trypanosoma cruzi and Toxoplasma gondii targeting farnesyl diphosphate synthase. | ||||
| Ref 552653 | Molecular mechanisms of action of bisphosphonates: current status. Clin Cancer Res. 2006 Oct 15;12(20 Pt 2):6222s-6230s. | ||||
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