DC73233 |
7HP349 |
Alintegimod (7HP349) is a small molecule activator of the integrins αLβ2 (LFA-1) and α4β1 (VLA-4). 7HP349 directly activates integrin cell adhesion receptors crucial for the generation of an immune response. |
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DC73234 |
A7B7C7 |
A7B7C7 (11-A7B7C7) is a potent Paxillin-α4 integrin binding antagonist with IC50 of 300 nM in vitro, decreases α4β1-mediated T cell migration. |
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DC73235 |
AXT107 |
AXT107 (AXT-107) mimetic peptide derived from collagen IV, binds integrins αvβ3 and α5β1 (Kd=1.29 and 2.21 nM), disrupts VEGFR2-β3 complex formation. |
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DC73236 |
GSK3335103
Featured
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GSK3335103 is a highly potent and orally bioavailable nonpeptidic αvβ6 integrin inhibitor with pIC50 of 8.0. GSK3335103 shows high desirable oral pharmacokinetic profiles in rat, dog, and minipig, with low to moderate clearance, moderate volumes of distributio, high to complete oral bioavailabilities and high solubility in all physiological media. |
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DC73237 |
GW559090 |
GW559090 is a potent, selective, competitive and high-affinity α4β1 integrin (VLA-4) antagonist with Kd of 0.19/1.04 nM for huamn/rat α4β1, respectively. |
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DC73238 |
IVL745 |
IVL745 (IVL-745) is a small molecule very late antigen (VLA-4) antagonist with IC50 of 20 nM and 2 nM for adhesion to VCAM-1 and fibronectin, respectively. |
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DC73239 |
MSR03 |
MSR03 is a potent, pure small molecule αVβ3 antagonist with IC50 of 1.5 uM for inhibition of adhesion of cells expressing human αVβ3 to immobilized fibrinogen. |
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DC73240 |
TBC4746 |
TBC 4746 (AVA4746) is a small molecule mimetic of VCAM-1 that binds VLA-4 on B-ALL cells with high affinity and efficiently blocks ligand-binding with VCAM-1 with EC50 of 38.52 nM. |
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DC73241 |
AM-1882
Featured
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AM-1882 (AM1882) is a potent, selective mitotic kinesin KIF18A inhibitor with IC50 of 230 nM in kinesin-8 microtubule (MT)-ATPase motor assays. |
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DC73242 |
AM-9022
Featured
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AM-9022 (AM9022) is a potent, selective and orally active mitotic kinesin KIF18A inhibitor with IC50 of 47 nM in kinesin-8 microtubule (MT)-ATPase motor assays. |
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DC73243 |
ALM201 |
ALM201 is a small 23 amino acid peptide derived from the FK506 binding protein FKBPL, a targeted microtubule binding agent which exhibits potent anti-angiogenic activity in vitro and in vivo. |
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DC73244 |
CH-2-77 |
CH-2-77 is a potent colchicine-binding site inhibitor (CBSI) targeting tubulin, shows potent anti-proliferative activity against a panel of cancer cells in vitro and efficacious anti-tumor effects in vivo. |
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DC73245 |
CH-2-77 analogue 60c |
CH-2-77 analogue 60c is a potent colchicine-binding site tubulin inhibitor, inhibits tubulin polymerization and is effective against P-glycoprotein-mediated multiple drug resistance and taxol resistance. |
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DC73246 |
EAPB02303 |
EAPB02303 (EAPB 02303) is a novel microtubule-disrupting agent with in-vivo activity in PDAC and in-vitro synergy with Paclitaxel, inhibits A375 melanoma cell line with IC50 of 3 nM. |
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DC73247 |
FiVe1
Featured
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FiVe1 is a vimentin binding small molecule that promotes vimentin disorganization and phosphorylation during metaphase, causes mitotic catastrophe, multinucleation, and the loss of stemness in cancer cells. |
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DC73248 |
KGP591 |
KGP591 is a small molecule inhibitor of tubulin polymerization with IC50 of 0.57 uM, exhibits cytotoxicity against the MCF-7 and MDA-MB-231 human breast cancer cell lines with GI50 of 320 and 102 nM, respectively. |
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DC73249 |
KGP618 |
KGP618 is the phosphate prodrug salt of KGP591, which is a small molecule inhibitor of tubulin polymerization with IC50 of 0.57 uM. |
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DC73250 |
Lexibulin |
An orally active tubulin polymerization inhibitor with potent cytotoxic and vascular disrupting activity in vitro and in vivo. |
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DC73251 |
R-huezole |
R-huezole is a phase-separating small molecule that forms liquid droplets to selectively sequester tubulin, enters cultured human cells and prevents cell mitosis by forming tubulin-concentrating condensates in cells. |
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DC73252 |
TN-2 |
TN-2 is a potent, dual tubulin/NRP1-targeting inhibitor with IC50 of 0.71 uM (tubulin polymerization) and 0.85 uM (NRP-1), inhibits proliferation and angiogenesis of tumor cells. |
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DC73253 |
BBC1115 |
BBC1115 is a novel chemotype inhibitor of bromodomain and extra-terminal motif (BET) proteins, displays broad binding across BDs of BET proteins. |
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DC73254 |
BI 1702135 |
BI 1702135 (Compound 4) is a potent SMARCA2 binder for targeted protein degradation (PROTAC) design as BI 1810284 (ACBI2, Cat. PC-20464). |
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DC73255 |
BI-4827 |
BI-4827 (BI 4827) is the negative control compound of BI-7190, which is a potent, selective chemical probe targeting the bromodomain of BPTF. |
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DC73256 |
BI-7190 |
BI-7190 (BI 7190) is a potent, selective chemical probe targeting the bromodomain of BPTF with binding Kd of 3.5 nM. |
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DC73257 |
CDD-787 |
CDD-787 is a highly potent, selective BET bromodomain 1 (BET BD1) inhibitor with IC50 of 2.1 and 3.3 nM for BRDT-BD1 and BRD4-BD1, respectively, with high selectivity (>3,000-fold) over BET BD2 proteins. |
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DC73258 |
CDD-956 |
CDD-956 is a highly potent, selective BET bromodomain 1 (BET BD1) inhibitor with IC50 of 2.1 and 4.4 nM for BRDT-BD1 and BRD4-BD1 respectively, with high selectivity (>500-fold) over BET BD2 proteins. |
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DC73259 |
CG13250 |
CG13250 (CG 13250, CG250) is a potent, selective and orally bioavailable BET bromodomain inhibitor with Kd of 44 nM (BRD4), IC50 of 1.1 uM (BRD4 BD1+BD2). |
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DC73260 |
CG223 |
CG223 (CG14223) is a potent and specific inhibitor of BET proteins with Kd of 45 nM for the C-terminal bromodomain of BRD3 (i.e. BRD3(2)) to 370 nM for the N-terminal bromodomain of BRDT (i.e. BRDT(1)). |
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DC73261 |
CN210 |
CN210 is a quinazoline-based BET family inhibitor with Kd value of 70 nM for BRD4 (BD1,2) and IC50 of 0.94 uM in MV4-11 viability assay. |
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DC73262 |
DDO-8926 |
DDO-8926 is a potent selective inhibitor of bromodomain and extra-terminal (BET) proteins with Ki values of 15 nM (BRD4 BD1) and 9.5 nM (BRD4 BD2). |
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