| nwamba # | Aha ngwaahịa | Nkọwa |
| CPD2809 | AMG-510 | AMG-510 bụ ihe mgbochi covalent KRAS G12C. AMG-510 na-ahọrọ nke ọma na-elekwasị anya na KRAS p.G12C mutant, na DNA, RNA ma ọ bụ protein, ma na-egbochi, site na nke a na-akọwabeghị ya, nkwupụta nke na/ma ọ bụ tumor cell na-egosi site na KRAS p.G12C mutant. Nke a nwere ike igbochi uto na KRAS p.G12C na-egosipụta mkpụrụ ndụ etuto |
| CPD100230 | JBJ-04-125-02 R-isomer | |
| CPD102300 | S-55746 | |
| CPD101235 | diABZI STING agonist-1 trihydrochloride | diABZI STING agonist-1 (trihydrochloride) bụ ihe mkpali nhọrọ nke interferon genes (STING) agonist nnabata, yana EC50s nke 130, 186 nM maka mmadụ na òké, n'otu n'otu. |
| CPD101234 | DiABZI STING agonist-1 (Tautomerism) | diABZI STING agonist-1 Tautomerism (mkpokọta 3) bụ ihe mkpali nhọrọ nke interferon genes (STING) agonist nnabata, yana EC50s nke 130, 186 nM maka mmadụ na òké, n'otu n'otu. |
| CPD101233 | diABZI STING agonist-1 | diABZI STING agonist-1 bụ ihe mkpali nhọrọ nke interferon genes (STING) agonist nnabata, yana EC50s nke 130, 186 nM maka mmadụ na òké, n'otu n'otu. |
| CPD101232 | agonist-4 | STING agonist-4 bụ ihe na-akpali akpali nke Interferon Genes (STING) agonist onye na-anabata ya na ihe mgbochi pụtara ìhè mgbe niile (IC50) nke 20 nM. STING agonist-4 bụ amidobenzimidazole (ABZI) jikọtara ya na-arụkọ ọrụ iji mepụta ABZI (diABZI) jikọtara ya na njikọta STING na ọrụ ekwentị. |
| CPD101231 | agonist-3 | STING agonist-3, nke ewepụtara na patent WO2017175147A1 (ihe atụ 10), bụ nhọrọ na-abụghị nucleotide obere-molecule agonist nwere pEC50 na pIC50 nke 7.5 na 9.5, n'otu n'otu. STING agonist-3 nwere mmetụta mgbochi tumor na-adịgide adịgide yana ikike dị ukwuu iji meziwanye ọgwụgwọ ọrịa kansa |
| CPD100904 | Voruciclib | Voruciclib, makwaara dị ka P1446A-05, bụ protein kinase inhibitor kpọmkwem maka cyclin-based kinase 4 (CDK4) nwere ọrụ antineoplastic. CDK4 inhibitor P1446A-05 na-egbochi mgbanwe oge nke CDK4-mediated G1-S, na-ejide ịnya igwe na igbochi uto mkpụrụ ndụ kansa. A na-achọta serine / threonine kinase CDK4 na mgbagwoju anya na ụdị D-ụdị G1 cyclins na ọ bụ kinase mbụ na-arụ ọrụ n'elu mkpali mitogenic, na-ahapụ mkpụrụ ndụ site na ọkwa nke quiescent n'ime G1 / S ịgba ígwè ịgba ígwè; E gosiputara ogige CDK-cyclin ka ọ na-eme ka phosphorylate ihe ntụgharị ederede retinoblastoma (Rb) n'oge G1, na-ewepụ histone deacetylase (HDAC) na igbochi mmegide transcriptional. |
| CPD100905 | Alvocidib | Alvocidib bụ ngwakọta N-methylpiperidinyl chlorophenyl flavone sịntetik. Dị ka onye na-egbochi cyclin-based kinase, alvocidib na-eme ka njide sel cell site na igbochi phosphorylation nke cyclin-dependent kinases (CDKs) na site na-achịkwa cyclin D1 na D3 okwu, na-akpata G1 cell cycle arrest na apoptosis. Onye nnọchi anya a bụkwa onye na-egbochi ọrụ adenosine triphosphate. Lelee maka nnwale ụlọ ọgwụ na-arụsi ọrụ ike ma ọ bụ nnwale ụlọ ọgwụ mechiri emechi site na iji nnọchite a. |
| CPD100906 | BS-181 | BS-181 bụ onye na-egbochi CDK nke ukwuu maka CDK7 nwere IC(50) nke 21 nmol/L. Nnwale nke CDK ndị ọzọ yana kinase 69 ọzọ gosiri na BS-181 na-egbochi CDK2 na mkpokọta dị ala karịa 1 micromol/L, na CDK2 na-egbochi 35-fold obere ike (IC(50) 880 nmol/L) karịa CDK7. N'ime mkpụrụ ndụ MCF-7, BS-181 gbochiri phosphorylation nke CDK7 substrates, na-akwalite njide okirikiri cell na apoptosis iji gbochie uto nke ahịrị mkpụrụ ndụ kansa, ma gosipụta mmetụta antitumor na vivo. |
| CPD100907 | Riviciclib | Riviciclib, nke a makwaara dị ka P276-00, bụ flavone na cyclin dabere kinase (CDK) inhibitor nwere ike antineoplastic ọrụ. P276-00 na-ahọrọ ma na-egbochi Cdk4/cyclin D1, Cdk1/cyclin B na Cdk9/cyclin T1, serine/threonine kinases nke na-arụ ọrụ dị mkpa na nhazi nke usoro cell na mgbasawanye cellular. Mgbochi nke kinases ndị a na-eduga na njide okirikiri cell n'oge mgbanwe G1/S, si otú ahụ na-eduga na ntinye nke apoptosis, na mgbochi nke mmụba cell tumor. |
| CPD100908 | MC180295 | MC180295 bụ onye na-egbochi CDK9 nke ukwuu (IC50 = 5 nM). (MC180295 nwere ọrụ mgbochi ọrịa cancer sara mbara na vitro ma dị irè na ụdị ọrịa cancer vivo. Ọzọkwa, mgbochi CDK9 na-eme ka ihe mgbochi mgbochi mgbochi α-PD-1 na vivo, na-eme ka ọ bụrụ ebumnuche magburu onwe ya maka ọgwụgwọ epigenetic nke ọrịa cancer. |
| 1073485-20-7 | LDC000067 | LDC000067 bụ ihe mgbochi CDK9 nwere ike na nhọrọ. LDC000067 amachibidoro ndegharị in vitro n'ụdị asọmpi ATP na dabere dose. Nkọwapụta mkpụrụ ndụ mkpụrụ ndụ nke e ji LDC000067 emeso ya gosipụtara mbelata nhọrọ nke mRNA dị mkpụmkpụ, gụnyere ndị na-achịkwa mkpa nke mgbasa na apoptosis. Nyocha nke njikọ de novo RNA na-atụ aro ọrụ dị oke mma nke CDK9. N'ọkwa molekụla na cellular, LDC000067 weputara mmetụta njirimara nke mgbochi CDK9 dị ka nkwụsịtụ RNA polymerase II na mkpụrụ ndụ ihe nketa na, nke kachasị mkpa, ntinye apoptosis na mkpụrụ ndụ kansa. LDC000067 na-egbochi ndenye P-TEFb dabere na in vitro. Na-ebute apoptosis in vitro na in vivo yana BI 894999. |
| CPD100910 | SEL120-34A | SEL120-34A bụ onye na-egbochi CDK8 dị ike ma họrọ nke na-arụ ọrụ na sel AML nwere ọkwa dị elu nke serine phosphorylation nke STAT1 na STAT5 ngalaba transactivation. EL120-34A na-egbochi phosphorylation nke STAT1 S727 na STAT5 S726 na mkpụrụ ndụ kansa na vitro. N'oge niile, a hụla ụkpụrụ nke STATs- na NUP98-HOXA9-edegharị ederede dabere dị ka usoro kachasị eme ihe na vivo. |
| CPD100501 | UNC2541 | UNC2541 bụ onye nwere ike na ihe mgbochi MerTK akọwapụtara nke na-egosipụta ọrụ inhibitory sub-micromolar na ELISA dabere na cell. Na mgbakwunye, a na-ekpebi usoro X-ray nke protein MerTK dị mgbagwoju anya yana 11 iji gosi na macrocycles ndị a na-ejikọta na akpa MerTK ATP. UNC2541 gosiri IC50 MerTH=4.4 nM; IC50 AXL = 120 nM; IC50 TYRO3 = 220 nM; IC50 FLT3 = 320 nM. |
| CPD100745 | RU-302 | RU-302 bụ pan-tam inhibitor akwụkwọ akụkọ, na-egbochi interface dị n'etiti tam ig1 ectodomain na gas6 lg ngalaba, na-egbochi ahịrị sel ndị nta akụkọ axl na ahịrị mkpụrụ ndụ kansa tam na-anabata ya. |
| CPD100744 | R916562 | |
| CPD100743 | Ningetinib-Tosylate | CT-053, nke a makwaara dị ka DE-120, bụ VEGF na PDGF inhibitor nwere ike maka ọgwụgwọ nke macular degeneration metụtara afọ mmiri. |
| CPD100742 | SGI-7079 | SGI-7079 bụ onye na-egbochi Axl dị ike ma họrọ nke nwere ọrụ mgbochi ọrịa kansa. SGI-7079 gbochiri ọrụ Axl nke ọma n'ihu Gas6 ligand exogenous. SGI-7079 gbochiri uto tumor na usoro dabere na dose. Axl bụ ebumnuche ọgwụgwọ nwere ike imeri nguzogide ihe mgbochi EGFR. |
| CPD100741 | 2-D08 | 2-D08 bụ flavone sịntetik nke na-egbochi sumoylation. 2-D08 gosipụtara mmetụta mgbochi mkpokọta na neuroprotective |
| CPD100740 | Dubermatinib | Dubermatinib, nke a makwaara dị ka TP-0903, bụ onye na-emechi AXL nwere ike na nhọrọ. TP-0903 na-ebute oke apoptosis na sel CLL B nwere ụkpụrụ LD50 nke oke nanomolar. Nchikota nke TP-0903 na BTK inhibitors na-abawanye CLL B-cell apoptosis AXL overexpression bụ isiokwu na-emegharị ugboro ugboro n'ọtụtụ ụdị tumo nke nwetara nguzogide dị iche iche. Ọgwụgwọ mkpụrụ ndụ kansa na TP-0903 na-atụgharị mesenchymal phenotype n'ọtụtụ ụdị ma mee ka mkpụrụ ndụ kansa nwee ike ịgwọ ya na ndị ọrụ ndị ọzọ ezubere iche. Nlekọta nke TP-0903 ma ọ bụ dịka otu onye ọrụ ma ọ bụ jikọtara ya na ndị na-egbochi BTK nwere ike ịdị irè n'ịgwọ ndị ọrịa nwere CLL. |
| CPD100739 | NPS-1034 | NPS-1034 bụ onye na-egbochi MET akwụkwọ akụkọ, nke na-egbochi nnabata MET na-arụ ọrụ yana mutant ya na-arụ ọrụ. NPS-1034, na-egbochi ụdị mutant dị iche iche nke MET yana HGF na-arụ ọrụ ụdị anụ ọhịa MET. NPS-1034 gbochiri mmụba nke mkpụrụ ndụ na-ekwupụta MET na-arụ ọrụ ma kwalite nlọghachi nke etuto ahụ sitere na mkpụrụ ndụ ndị dị otú ahụ na ụdị xenograft òké site na omume mgbochi angiogenic na pro-apoptotic. NPS-1034 gbochiri HGF-akpali akpali nke nrịbama MET na ọnụnọ ma ọ bụ enweghị serum. N'ụzọ doro anya, NPS-1034 gbochiri ụdị MET atọ nke na-eguzogide MET inhibitors SU11274, NVP-BVU972, na PHA665752. |
| CPD100738 | Glesatinib | Glesatinib, nke a makwaara dị ka MGCD-265, bụ ihe a na-ahụ maka ọnụ, obere molecule, multitargeted tyrosine kinase inhibitor nwere ọrụ antineoplastic. MGCD265 na-ejikọta ma na-egbochi phosphorylation nke ọtụtụ tyrosine kinases (RTKs), gụnyere c-Met receptor ( hepatocyte growth factor receptor); onye na-anabata Tek / Tie-2; vascular endothelial growth factor receptor (VEGFR) ụdị 1, 2, na 3; na macrophage-na-akpali akpali 1 receptor (MST1R ma ọ bụ RON). |
