SK&F 107260: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 164393 |
| CHEMBL ID | 18734 |
| MeSH ID | M0229435 |
| Synonym |
|---|
| sk&f 107260 |
| 136620-00-3 |
| [(7s,13s)-13-(3-guanidino-propyl)-14-methyl-6,9,12,15-tetraoxo-6,7,8,9,10,11,12,13,14,15-decahydro-5h-20,21-dithia-5,8,11,14-tetraaza-dibenzo[a,e]cycloheptadecen-7-yl]-acetic acid |
| [(6s,13s)-13-(3-guanidino-propyl)-14-methyl-6,9,12,15-tetraoxo-6,7,8,9,10,11,12,13,14,15-decahydro-5h-20,21-dithia-5,8,11,14-tetraaza-dibenzo[a,e]cycloheptadecen-7-yl]-acetic acid |
| bdbm50036088 |
| [13-(3-guanidino-propyl)-14-methyl-6,9,12,15-tetraoxo-6,7,8,9,10,11,12,13,14,15-decahydro-5h-20,21-dithia-5,8,11,14-tetraaza-dibenzo[a,e]cycloheptadecen-7-yl]-acetic acid (sk&f 107260) |
| CHEMBL18734 , |
| skf-107260 |
| n2-(2-mercaptobenzoyl)-n2-methyl-l-arginylglycyl-n-(2-mercaptophenyl)-l-alpha-asparagine cyclic(1-3)-disulfide |
| cyclo-s,s-(mba-(n(alpha)-me)arg-gly-asp-man) |
| sk&f-107260 |
| l-alpha-asparagine, n2-(2-mercaptobenzoyl)-n2-methyl-l-arginylglycyl-n-(2-mercaptophenyl)-, cyclic(1-3)-disulfide |
| skf 107260 |
| cyclo-s,s-(2-mercaptobenzoyl-n(alpha)-methylarginyl-glycyl-aspartyl-2-mercaptophenylamide) |
| DTXSID70159857 |
| 2-[(12s,18s)-18-[3-(diaminomethylideneamino)propyl]-19-methyl-11,14,17,20-tetraoxo-2,3-dithia-10,13,16,19-tetrazatricyclo[19.4.0.04,9]pentacosa-1(25),4,6,8,21,23-hexaen-12-yl]acetic acid |
| bdbm50230131 |
| 2-((7s,13s)-13-(3-guanidinopropyl)-14-methyl-6,9,12,15-tetraoxo-6,7,8,9,10,11,12,13,14,15-decahydro-5h-dibenzo[c,p][1,2]dithia[5,8,11,14]tetraazacycloheptadecin-7-yl)acetic acid |
| l-alpha-asparagine, n2-(2-mercaptobenzoyl)-n2-methyl-l-arginylglycyl-n-(2-mercaptophenyl)-, cyclic (1-->3)-disulfide |
| Excerpt | Reference | Relevance |
|---|---|---|
| " Comparison of the iv and id inhibition curves suggests an apparent bioavailability of approximately 10%." | ( Design of a potent and orally active nonpeptide platelet fibrinogen receptor (GPIIb/IIIa) antagonist. Ali, FE; Allen, AC; Bondinell, WE; de Brosse, CW; Eggleston, DS; Erhard, KF; Haltiwanger, RC; Huffman, WF; Keenan, RM; Miller, WH, 1994) | 0.29 |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Integrin beta-3 | Homo sapiens (human) | Ki | 0.0031 | 0.0010 | 0.9845 | 9.1400 | AID217446; AID220616; AID32987; AID32988; AID73004; AID73149 |
| Integrin alpha-V | Homo sapiens (human) | Ki | 0.0035 | 0.0010 | 0.0021 | 0.0035 | AID217446; AID220616 |
| Integrin alpha-IIb | Homo sapiens (human) | Ki | 0.0029 | 0.0020 | 2.3352 | 9.1400 | AID32987; AID32988; AID73004; AID73149 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID73004 | Inhibition of [3H]-107260 binding to purified GPIIb/IIIa of human platelets | 1992 | Journal of medicinal chemistry, Oct-16, Volume: 35, Issue:21 | Design and synthesis of a C7 mimetic for the predicted gamma-turn conformation found in several constrained RGD antagonists. |
| AID220616 | Inhibition of binding to alphaV-beta3 integrin | 2003 | Journal of medicinal chemistry, Oct-09, Volume: 46, Issue:21 | Docking studies on alphavbeta3 integrin ligands: pharmacophore refinement and implications for drug design. |
| AID32988 | Inhibition of [3H]-SKF- 107260 binding to purified alphaIIb-beta3 integrin of human platelets | 1995 | Journal of medicinal chemistry, Jan-06, Volume: 38, Issue:1 | Potent non-peptide fibrinogen receptor antagonists which present an alternative pharmacophore. |
| AID161426 | Inhibition of ADP-induced platelet aggregation in canine platelet-rich plasma | 1992 | Journal of medicinal chemistry, Oct-16, Volume: 35, Issue:21 | Design and synthesis of a C7 mimetic for the predicted gamma-turn conformation found in several constrained RGD antagonists. |
| AID217446 | Affinity for vitronectin receptor, integrin alphaV-beta3 | 1997 | Journal of medicinal chemistry, Jul-18, Volume: 40, Issue:15 | Discovery of potent nonpeptide vitronectin receptor (alpha v beta 3) antagonists. |
| AID32987 | Inhibition of binding to purified integrin alphaIIb-beta3 of human platelets | 1996 | Journal of medicinal chemistry, Dec-06, Volume: 39, Issue:25 | Potent, selective, orally active 3-oxo-1,4-benzodiazepine GPIIb/IIIa integrin antagonists. |
| AID229242 | Inhibition of vitronectin receptor binding | 2000 | Journal of medicinal chemistry, Sep-21, Volume: 43, Issue:19 | Platelet glycoprotein IIb-IIIa antagonists as prototypical integrin blockers: novel parenteral and potential oral antithrombotic agents. |
| AID158229 | In vitro Inhibitory activity against patelet aggregation in human platelet-rich plasma induced by ADP | 1996 | Journal of medicinal chemistry, Dec-06, Volume: 39, Issue:25 | Potent, selective, orally active 3-oxo-1,4-benzodiazepine GPIIb/IIIa integrin antagonists. |
| AID73149 | Affinity for platelet fibrinogen receptor, integrin alpha IIb/beta3 | 1997 | Journal of medicinal chemistry, Jul-18, Volume: 40, Issue:15 | Discovery of potent nonpeptide vitronectin receptor (alpha v beta 3) antagonists. |
| AID158084 | Antiaggregatory activity against human platelet-rich plasma induced by ADP | 1995 | Journal of medicinal chemistry, Jan-06, Volume: 38, Issue:1 | Potent non-peptide fibrinogen receptor antagonists which present an alternative pharmacophore. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 9 (81.82) | 18.2507 |
| 2000's | 2 (18.18) | 29.6817 |
| 2010's | 0 (0.00) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.
| This Compound (11.68) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 1 (9.09%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 10 (90.91%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||