Discoidin domain receptors (DDRs) are members of the transmembrane receptor tyrosine kinase (RTK) superfamily which are distinguished from others by the presence of a discoidin motif in the extracellular domain and their utilization of collagens as internal ligands. DDR1 and DDR2, two types of DDRs with different expression patterns and ligand preferences, have been discovered.
DDRs bind to collagen and then transmit cellular signaling that is involved in a number of different cell processes, such as adhesion, proliferation, differentiation, migration, and matrix homeostasis. Atherosclerosis, inflammation, cancer, and tissue fibrosis have all been linked to altered DDR function that results from either mutations or overexpression. New small molecule inhibitors that target the receptors are being sought after because DDRs have been identified as novel potential molecular targets for drug discovery.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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V4169 | BAY-826 | 1448316-08-2 | BAY-826 is a novel, highly potent, selective and orally available small molecule TIE-2 inhibitor withKdof 1.6 nM, respectively. |
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V1882 | DDR1-IN-1 | 1449685-96-4 | DDR1-IN-1 is a potent and selective discoidin domain receptor 1 (DDR1) receptor tyrosine kinase inhibitor with IC50 of 105 nM, and is about 3-fold selectivity over DDR2. |
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V69326 | DDR1-IN-4 | 2125676-13-1 | DDR1-IN-4 (Compound 2.45) is a potent and specific inhibitor of Discopeptide Domain Receptor 1 (DDR1) autophosphorylation with IC50s of 29 nM and 1.9 μM for DDR1 and DDR2, respectively. |
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V69328 | DDR1-IN-5 | 2416022-90-5 | DDR1-IN-5 is a selective discoid domain receptor family member 1 (DDR1) inhibitor (antagonist) with IC50 of 7.36 nM. |
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V69327 | DDR1-IN-6 | 2416021-47-9 | DDR1-IN-6 is a selective discoid domain receptor family member 1 (DDR1) inhibitor (antagonist) with IC50 of 9.72 nM. |
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V69329 | DDR1/2 inhibitor-2 | 2908756-11-4 | DDR1/2 inhibitor-2 (Example 31) is a DDR1/DDR2 inhibitor (antagonist) with IC50 of less than 100 nM. |
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V69325 | DDR2-IN-1 | 1573053-23-2 | DDR2-IN-1 is a potent DDR2 inhibitor (antagonist) with IC50 of 26 nM. |
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V83244 | Dual DDR1 and DDR2 inhibitor 5n | 2241813-33-0 | Dual DDR1 and DDR2 inhibitor 5n is a dual inhibitor of Discoidin domain receptor DDR1/DDR2 with Kd of 7.9 and 8.0 nM, IC50 of 9.4 and 20.4 nM, repectively. |
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