- Uniprot ID:
- Q9NYV4
- Q96SZ6
- Q96GD4
- Q91820
- Q7KZI7
- Q2M2I8
- Q14289
- Q14004
- Q13131
- Q08881
- Q06187
- Q05397
- Q00537
- Q00534
- P53671
- P51451
- P50750
- P50613
- P42680
- P36888
- P35991
- P30291
- P24941
- P16591
- P11802
- P07332
- P06239
- O75385
- O14976
Target: CDK12 Cyclin-dependent kinase 12 Q9NYV4 Homo sapiens
MW: 931.47 Hbond donors: 5 Hbond acceptors: 16 cLogP: 3.58 TPSA: 233.60 SMILES: show CC(C)S(=O)(=O)c1ccccc1Nc1nc(Nc2ccc(N3CCN(CCOCCOCCNC(=O)CNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)cc2)ncc1Cl Linker type: Other Incubation time (hours): 4 Cells: MOLT-4, MOLM14 IC50: = 10.3 nM DC50: < 100 nM Dmax: > 85 % Off-targets reported?: INCENP, NDUFAB1, CCNH, CCNK, and IKZF1 Comments: General kinase PROTAC, DCmax is for the most degraded kinase. IC50 of the ligand is for 193 kinases in the panel. IC50 of the PROTAC is by FLT3 kinase activity. Contributed by: Ronen Gabizon |
Target: CDK5RAP1 Mitochondrial tRNA methylthiotransferase CDK5RAP1 Q96SZ6 Homo sapiens
MW: 931.47 Hbond donors: 5 Hbond acceptors: 16 cLogP: 3.58 TPSA: 233.60 SMILES: show CC(C)S(=O)(=O)c1ccccc1Nc1nc(Nc2ccc(N3CCN(CCOCCOCCNC(=O)CNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)cc2)ncc1Cl Linker type: Other Incubation time (hours): 4 Cells: MOLT-4, MOLM14 IC50: = 10.3 nM DC50: < 100 nM Dmax: > 85 % Off-targets reported?: INCENP, NDUFAB1, CCNH, CCNK, and IKZF1 Comments: General kinase PROTAC, DCmax is for the most degraded kinase. IC50 of the ligand is for 193 kinases in the panel. IC50 of the PROTAC is by FLT3 kinase activity. Contributed by: Ronen Gabizon |
Target: AURKB Aurora kinase B Q96GD4 Homo sapiens
MW: 931.47 Hbond donors: 5 Hbond acceptors: 16 cLogP: 3.58 TPSA: 233.60 SMILES: show CC(C)S(=O)(=O)c1ccccc1Nc1nc(Nc2ccc(N3CCN(CCOCCOCCNC(=O)CNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)cc2)ncc1Cl Linker type: Other Incubation time (hours): 4 Cells: MOLT-4, MOLM14 IC50: = 10.3 nM DC50: < 100 nM Dmax: > 85 % Off-targets reported?: INCENP, NDUFAB1, CCNH, CCNK, and IKZF1 Comments: General kinase PROTAC, DCmax is for the most degraded kinase. IC50 of the ligand is for 193 kinases in the panel. IC50 of the PROTAC is by FLT3 kinase activity. Contributed by: Ronen Gabizon |
Target: aurka-a Aurora kinase A-A Q91820 Homo sapiens
MW: 931.47 Hbond donors: 5 Hbond acceptors: 16 cLogP: 3.58 TPSA: 233.60 SMILES: show CC(C)S(=O)(=O)c1ccccc1Nc1nc(Nc2ccc(N3CCN(CCOCCOCCNC(=O)CNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)cc2)ncc1Cl Linker type: Other Incubation time (hours): 4 Cells: MOLT-4, MOLM14 IC50: = 10.3 nM DC50: < 100 nM Dmax: > 85 % Off-targets reported?: INCENP, NDUFAB1, CCNH, CCNK, and IKZF1 Comments: General kinase PROTAC, DCmax is for the most degraded kinase. IC50 of the ligand is for 193 kinases in the panel. IC50 of the PROTAC is by FLT3 kinase activity. Contributed by: Ronen Gabizon |
Target: MARK2 Serine/threonine-protein kinase MARK2 Q7KZI7 Homo sapiens
MW: 931.47 Hbond donors: 5 Hbond acceptors: 16 cLogP: 3.58 TPSA: 233.60 SMILES: show CC(C)S(=O)(=O)c1ccccc1Nc1nc(Nc2ccc(N3CCN(CCOCCOCCNC(=O)CNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)cc2)ncc1Cl Linker type: Other Incubation time (hours): 4 Cells: MOLT-4, MOLM14 IC50: = 10.3 nM DC50: < 100 nM Dmax: > 85 % Off-targets reported?: INCENP, NDUFAB1, CCNH, CCNK, and IKZF1 Comments: General kinase PROTAC, DCmax is for the most degraded kinase. IC50 of the ligand is for 193 kinases in the panel. IC50 of the PROTAC is by FLT3 kinase activity. Contributed by: Ronen Gabizon |
Target: AAK1 AP2-associated protein kinase 1 Q2M2I8 Homo sapiens
MW: 931.47 Hbond donors: 5 Hbond acceptors: 16 cLogP: 3.58 TPSA: 233.60 SMILES: show CC(C)S(=O)(=O)c1ccccc1Nc1nc(Nc2ccc(N3CCN(CCOCCOCCNC(=O)CNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)cc2)ncc1Cl Linker type: Other Incubation time (hours): 4 Cells: MOLT-4, MOLM14 IC50: = 10.3 nM DC50: < 100 nM Dmax: > 85 % Off-targets reported?: INCENP, NDUFAB1, CCNH, CCNK, and IKZF1 Comments: General kinase PROTAC, DCmax is for the most degraded kinase. IC50 of the ligand is for 193 kinases in the panel. IC50 of the PROTAC is by FLT3 kinase activity. Contributed by: Ronen Gabizon |
Target: PTK2B Protein-tyrosine kinase 2-beta Q14289 Homo sapiens
MW: 931.47 Hbond donors: 5 Hbond acceptors: 16 cLogP: 3.58 TPSA: 233.60 SMILES: show CC(C)S(=O)(=O)c1ccccc1Nc1nc(Nc2ccc(N3CCN(CCOCCOCCNC(=O)CNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)cc2)ncc1Cl Linker type: Other Incubation time (hours): 4 Cells: MOLT-4, MOLM14 IC50: = 10.3 nM DC50: < 100 nM Dmax: > 85 % Off-targets reported?: INCENP, NDUFAB1, CCNH, CCNK, and IKZF1 Comments: General kinase PROTAC, DCmax is for the most degraded kinase. IC50 of the ligand is for 193 kinases in the panel. IC50 of the PROTAC is by FLT3 kinase activity. Contributed by: Ronen Gabizon |
Target: CDK13 Cyclin-dependent kinase 13 Q14004 Homo sapiens
MW: 931.47 Hbond donors: 5 Hbond acceptors: 16 cLogP: 3.58 TPSA: 233.60 SMILES: show CC(C)S(=O)(=O)c1ccccc1Nc1nc(Nc2ccc(N3CCN(CCOCCOCCNC(=O)CNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)cc2)ncc1Cl Linker type: Other Incubation time (hours): 4 Cells: MOLT-4, MOLM14 IC50: = 10.3 nM DC50: < 100 nM Dmax: > 85 % Off-targets reported?: INCENP, NDUFAB1, CCNH, CCNK, and IKZF1 Comments: General kinase PROTAC, DCmax is for the most degraded kinase. IC50 of the ligand is for 193 kinases in the panel. IC50 of the PROTAC is by FLT3 kinase activity. Contributed by: Ronen Gabizon |
Target: PRKAA1 5'-AMP-activated protein kinase catalytic subunit alpha-1 Q13131 Homo sapiens
MW: 931.47 Hbond donors: 5 Hbond acceptors: 16 cLogP: 3.58 TPSA: 233.60 SMILES: show CC(C)S(=O)(=O)c1ccccc1Nc1nc(Nc2ccc(N3CCN(CCOCCOCCNC(=O)CNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)cc2)ncc1Cl Linker type: Other Incubation time (hours): 4 Cells: MOLT-4, MOLM14 IC50: = 10.3 nM DC50: < 100 nM Dmax: > 85 % Off-targets reported?: INCENP, NDUFAB1, CCNH, CCNK, and IKZF1 Comments: General kinase PROTAC, DCmax is for the most degraded kinase. IC50 of the ligand is for 193 kinases in the panel. IC50 of the PROTAC is by FLT3 kinase activity. Contributed by: Ronen Gabizon |
Target: ITK Tyrosine-protein kinase ITK/TSK Q08881 Homo sapiens
MW: 931.47 Hbond donors: 5 Hbond acceptors: 16 cLogP: 3.58 TPSA: 233.60 SMILES: show CC(C)S(=O)(=O)c1ccccc1Nc1nc(Nc2ccc(N3CCN(CCOCCOCCNC(=O)CNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)cc2)ncc1Cl Linker type: Other Incubation time (hours): 4 Cells: MOLT-4, MOLM14 IC50: = 10.3 nM DC50: < 100 nM Dmax: > 85 % Off-targets reported?: INCENP, NDUFAB1, CCNH, CCNK, and IKZF1 Comments: General kinase PROTAC, DCmax is for the most degraded kinase. IC50 of the ligand is for 193 kinases in the panel. IC50 of the PROTAC is by FLT3 kinase activity. Contributed by: Ronen Gabizon |
Target: BTK Tyrosine-protein kinase BTK Q06187 Homo sapiens
MW: 903.82 Hbond donors: 3 Hbond acceptors: 15 cLogP: 5.11 TPSA: 196.92 SMILES: show COc1cc(Nc2c(C#N)cnc3cc(OCCCN4CCN(CCOCCOCCNc5cccc6c5C(=O)N(C5CCC(=O)NC5=O)C6=O)CC4)c(OC)cc23)c(Cl)cc1Cl Linker type: Other Incubation time (hours): 4 Cells: MOLM14, MV4-11 DC50: ~ 100 nM Dmax: ~ 50 % Off-targets reported?: No Comments: IC50 of ligand is inhibitory - data from Selleckchem. EC50 of the lidand is Src-dependent cell proliferation - data from Selleckchem. Contributed by: Ronen Gabizon |
MW: 1,033.16 Hbond donors: 5 Hbond acceptors: 17 cLogP: 3.96 TPSA: 238.77 SMILES: show Cc1cc(C2CC2)cc2ccn(-c3cccc(-c4cc(Nc5ccc(N6CCN(CCOCCOCCNC(=O)CNc7cccc8c7C(=O)N(C7CCC(=O)NC7=O)C8=O)CC6)cn5)c(=O)n(C)c4)c3CO)c(=O)c12 Linker type: Other Incubation time (hours): 4 Cells: MOLM14 DC50: < 40 nM Dmax: ~ 90 % Off-targets reported?: No Comments: IC50 of ligand is 4 nM (BTK inhibition)/ 0.3 nM (binding). EC50 of ligand is 20-30 nM (B-cell signaling). Contributed by: Ronen Gabizon |
Target: PTK2 Focal adhesion kinase 1 Q05397 Homo sapiens
MW: 931.47 Hbond donors: 5 Hbond acceptors: 16 cLogP: 3.58 TPSA: 233.60 SMILES: show CC(C)S(=O)(=O)c1ccccc1Nc1nc(Nc2ccc(N3CCN(CCOCCOCCNC(=O)CNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)cc2)ncc1Cl Linker type: Other Incubation time (hours): 4 Cells: MOLT-4, MOLM14 IC50: = 10.3 nM DC50: < 100 nM Dmax: > 85 % Off-targets reported?: INCENP, NDUFAB1, CCNH, CCNK, and IKZF1 Comments: General kinase PROTAC, DCmax is for the most degraded kinase. IC50 of the ligand is for 193 kinases in the panel. IC50 of the PROTAC is by FLT3 kinase activity. Contributed by: Ronen Gabizon |
Target: CDK17 Cyclin-dependent kinase 17 Q00537 Homo sapiens
MW: 931.47 Hbond donors: 5 Hbond acceptors: 16 cLogP: 3.58 TPSA: 233.60 SMILES: show CC(C)S(=O)(=O)c1ccccc1Nc1nc(Nc2ccc(N3CCN(CCOCCOCCNC(=O)CNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)cc2)ncc1Cl Linker type: Other Incubation time (hours): 4 Cells: MOLT-4, MOLM14 IC50: = 10.3 nM DC50: < 100 nM Dmax: > 85 % Off-targets reported?: INCENP, NDUFAB1, CCNH, CCNK, and IKZF1 Comments: General kinase PROTAC, DCmax is for the most degraded kinase. IC50 of the ligand is for 193 kinases in the panel. IC50 of the PROTAC is by FLT3 kinase activity. Contributed by: Ronen Gabizon |
Target: CDK6 Cyclin-dependent kinase 6 Q00534 Homo sapiens
MW: 931.47 Hbond donors: 5 Hbond acceptors: 16 cLogP: 3.58 TPSA: 233.60 SMILES: show CC(C)S(=O)(=O)c1ccccc1Nc1nc(Nc2ccc(N3CCN(CCOCCOCCNC(=O)CNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)cc2)ncc1Cl Linker type: Other Incubation time (hours): 4 Cells: MOLT-4, MOLM14 IC50: = 10.3 nM DC50: < 100 nM Dmax: > 85 % Off-targets reported?: INCENP, NDUFAB1, CCNH, CCNK, and IKZF1 Comments: General kinase PROTAC, DCmax is for the most degraded kinase. IC50 of the ligand is for 193 kinases in the panel. IC50 of the PROTAC is by FLT3 kinase activity. Contributed by: Ronen Gabizon |
Target: LIMK2 LIM domain kinase 2 P53671 Homo sapiens
MW: 931.47 Hbond donors: 5 Hbond acceptors: 16 cLogP: 3.58 TPSA: 233.60 SMILES: show CC(C)S(=O)(=O)c1ccccc1Nc1nc(Nc2ccc(N3CCN(CCOCCOCCNC(=O)CNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)cc2)ncc1Cl Linker type: Other Incubation time (hours): 4 Cells: MOLT-4, MOLM14 IC50: = 10.3 nM DC50: < 100 nM Dmax: > 85 % Off-targets reported?: INCENP, NDUFAB1, CCNH, CCNK, and IKZF1 Comments: General kinase PROTAC, DCmax is for the most degraded kinase. IC50 of the ligand is for 193 kinases in the panel. IC50 of the PROTAC is by FLT3 kinase activity. Contributed by: Ronen Gabizon |
Target: BLK Tyrosine-protein kinase Blk P51451 Homo sapiens
MW: 931.47 Hbond donors: 5 Hbond acceptors: 16 cLogP: 3.58 TPSA: 233.60 SMILES: show CC(C)S(=O)(=O)c1ccccc1Nc1nc(Nc2ccc(N3CCN(CCOCCOCCNC(=O)CNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)cc2)ncc1Cl Linker type: Other Incubation time (hours): 4 Cells: MOLT-4, MOLM14 IC50: = 10.3 nM DC50: < 100 nM Dmax: > 85 % Off-targets reported?: INCENP, NDUFAB1, CCNH, CCNK, and IKZF1 Comments: General kinase PROTAC, DCmax is for the most degraded kinase. IC50 of the ligand is for 193 kinases in the panel. IC50 of the PROTAC is by FLT3 kinase activity. Contributed by: Ronen Gabizon |
Target: CDK9 Cyclin-dependent kinase 9 P50750 Homo sapiens
MW: 931.47 Hbond donors: 5 Hbond acceptors: 16 cLogP: 3.58 TPSA: 233.60 SMILES: show CC(C)S(=O)(=O)c1ccccc1Nc1nc(Nc2ccc(N3CCN(CCOCCOCCNC(=O)CNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)cc2)ncc1Cl Linker type: Other Incubation time (hours): 4 Cells: MOLT-4, MOLM14 IC50: = 10.3 nM DC50: < 100 nM Dmax: > 85 % Off-targets reported?: INCENP, NDUFAB1, CCNH, CCNK, and IKZF1 Comments: General kinase PROTAC, DCmax is for the most degraded kinase. IC50 of the ligand is for 193 kinases in the panel. IC50 of the PROTAC is by FLT3 kinase activity. Contributed by: Ronen Gabizon |
Target: CDK7 Cyclin-dependent kinase 7 P50613 Homo sapiens
MW: 931.47 Hbond donors: 5 Hbond acceptors: 16 cLogP: 3.58 TPSA: 233.60 SMILES: show CC(C)S(=O)(=O)c1ccccc1Nc1nc(Nc2ccc(N3CCN(CCOCCOCCNC(=O)CNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)cc2)ncc1Cl Linker type: Other Incubation time (hours): 4 Cells: MOLT-4, MOLM14 IC50: = 10.3 nM DC50: < 100 nM Dmax: > 85 % Off-targets reported?: INCENP, NDUFAB1, CCNH, CCNK, and IKZF1 Comments: General kinase PROTAC, DCmax is for the most degraded kinase. IC50 of the ligand is for 193 kinases in the panel. IC50 of the PROTAC is by FLT3 kinase activity. Contributed by: Ronen Gabizon |
Target: TEC Tyrosine-protein kinase Tec P42680 Homo sapiens
MW: 931.47 Hbond donors: 5 Hbond acceptors: 16 cLogP: 3.58 TPSA: 233.60 SMILES: show CC(C)S(=O)(=O)c1ccccc1Nc1nc(Nc2ccc(N3CCN(CCOCCOCCNC(=O)CNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)cc2)ncc1Cl Linker type: Other Incubation time (hours): 4 Cells: MOLT-4, MOLM14 IC50: = 10.3 nM DC50: < 100 nM Dmax: > 85 % Off-targets reported?: INCENP, NDUFAB1, CCNH, CCNK, and IKZF1 Comments: General kinase PROTAC, DCmax is for the most degraded kinase. IC50 of the ligand is for 193 kinases in the panel. IC50 of the PROTAC is by FLT3 kinase activity. Contributed by: Ronen Gabizon |
Target: FLT3 Receptor-type tyrosine-protein kinase FLT3 P36888 Homo sapiens
MW: 936.02 Hbond donors: 5 Hbond acceptors: 16 cLogP: 5.20 TPSA: 246.06 SMILES: show CC(C)(C)c1cc(NC(=O)Nc2ccc(-c3cn4c(n3)sc3cc(OCCOCCOCCOCCNC(=O)CNc5cccc6c5C(=O)N(C5CCC(=O)NC5=O)C6=O)ccc34)cc2)no1 Linker type: PEG Incubation time (hours): 12 Cells: MOLM14, MV4-11 DC50: < 10 nM Dmax: ~ 100 % Off-targets reported?: No; confirmed that AURKA, BTK and PTK2B are not degraded Comments: Dmax is difficult to quantify because AC220 raises FLT3 expression levels. IC50 of ligand is 1.6 nM (binding); 1.1-4 (activity). EC50 of ligand is measured on MOLM-14 cell lines. EC50 of PROTAC was measured on MOLM-14 cell lines. Contributed by: Ronen Gabizon MW: 1,004.14 Hbond donors: 5 Hbond acceptors: 17 cLogP: 4.80 TPSA: 243.31 SMILES: show CC(C)(C)c1cc(NC(=O)Nc2ccc(-c3cn4c(n3)sc3cc(OCCN5CCN(CCOCCOCCNC(=O)CNc6cccc7c6C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)ccc34)cc2)no1 Linker type: Other Incubation time (hours): 12 Cells: MOLM14, MV4-11 DC50: < 10 nM Dmax: ~ 100 % Off-targets reported?: No; confirmed that AURKA, BTK and PTK2B are not degraded Comments: Dmax is difficult to quantify because AC220 raises FLT3 expression levels. IC50 of ligand is 1.6 nM (binding); 1.1-4 (activity). EC50 of ligand is measured on MOLM-14 cell lines. EC50 of PROTAC was measured on MOLM-14 cell lines. Contributed by: Ronen Gabizon MW: 891.96 Hbond donors: 5 Hbond acceptors: 15 cLogP: 5.19 TPSA: 236.83 SMILES: show CC(C)(C)c1cc(NC(=O)Nc2ccc(-c3cn4c(n3)sc3cc(OCCOCCOCCNC(=O)CNc5cccc6c5C(=O)N(C5CCC(=O)NC5=O)C6=O)ccc34)cc2)no1 Linker type: PEG Incubation time (hours): 12 Cells: MOLM14, MV4-11 Off-targets reported?: No Comments: IC50 of ligand is 1.6 nM (binding); 1.1-4 (activity). EC50 of ligand is measured on MOLM-14 cell lines Contributed by: Ronen Gabizon |
MW: 931.47 Hbond donors: 5 Hbond acceptors: 16 cLogP: 3.58 TPSA: 233.60 SMILES: show CC(C)S(=O)(=O)c1ccccc1Nc1nc(Nc2ccc(N3CCN(CCOCCOCCNC(=O)CNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)cc2)ncc1Cl Linker type: Other Incubation time (hours): 4 Cells: MOLT-4, MOLM14 IC50: = 10.3 nM DC50: < 100 nM Dmax: > 85 % Off-targets reported?: INCENP, NDUFAB1, CCNH, CCNK, and IKZF1 Comments: General kinase PROTAC, DCmax is for the most degraded kinase. IC50 of the ligand is for 193 kinases in the panel. IC50 of the PROTAC is by FLT3 kinase activity. Contributed by: Ronen Gabizon |
MW: 1,048.17 Hbond donors: 7 Hbond acceptors: 16 cLogP: 4.09 TPSA: 289.28 SMILES: show CC(C)(C)/C(O)=C/C(=N)N[N+](=O)Nc1ccc(-c2cn3c(n2)sc2cc(OCCN4CCN(C(=O)CCC(=O)NCCCCNC(=O)COc5cccc6c5C(=O)N(C5CCC(=O)NC5=O)C6=O)CC4)ccc23)cc1 Linker type: Other Incubation time (hours): 12 Cells: MOLM14, MV4-11 Off-targets reported?: No Comments: IC50 of ligand is 1.6 nM (binding); 1.1-4 (activity). EC50 of ligand is measured on MOLM-14 cell lines Contributed by: Ronen Gabizon MW: 1,002.12 Hbond donors: 5 Hbond acceptors: 16 cLogP: 4.63 TPSA: 251.15 SMILES: show CC(C)(C)c1cc(NC(=O)Nc2ccc(-c3cn4c(n3)sc3cc(OCCN5CCN(CC(=O)NCCCCNC(=O)COc6cccc7c6C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)ccc34)cc2)no1 Linker type: Other Incubation time (hours): 12 Cells: MOLM14, MV4-11 Off-targets reported?: No Comments: IC50 of ligand is 1.6 nM (binding); 1.1-4 (activity). EC50 of ligand is measured on MOLM-14 cell lines Contributed by: Ronen Gabizon MW: 1,058.23 Hbond donors: 5 Hbond acceptors: 16 cLogP: 6.20 TPSA: 251.15 SMILES: show CC(C)(C)c1cc(NC(=O)Nc2ccc(-c3cn4c(n3)sc3cc(OCCN5CCN(CC(=O)NCCCCCCCCNC(=O)COc6cccc7c6C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)ccc34)cc2)no1 Linker type: Other Incubation time (hours): 12 Cells: MOLM14, MV4-11 Off-targets reported?: No Comments: IC50 of ligand is 1.6 nM (binding); 1.1-4 (activity). EC50 of ligand is measured on MOLM-14 cell lines Contributed by: Ronen Gabizon MW: 1,134.28 Hbond donors: 5 Hbond acceptors: 19 cLogP: 4.68 TPSA: 278.84 SMILES: show CC(C)(C)c1cc(NC(=O)Nc2ccc(-c3cn4c(n3)sc3cc(OCCN5CCN(CC(=O)NCCCOCCOCCOCCCNC(=O)COc6cccc7c6C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)ccc34)cc2)no1 Linker type: Other Incubation time (hours): 12 Cells: MOLM14, MV4-11 Off-targets reported?: No Comments: IC50 of ligand is 1.6 nM (binding); 1.1-4 (activity). EC50 of ligand is measured on MOLM-14 cell lines Contributed by: Ronen Gabizon MW: 1,100.27 Hbond donors: 5 Hbond acceptors: 16 cLogP: 6.50 TPSA: 268.22 SMILES: show CC(C)(C)c1cc(NC(=O)Nc2ccc(-c3cn4c(n3)sc3cc(OCCN5CCN(C(=O)CCC(=O)NCCCCCCCCNC(=O)COc6cccc7c6C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)ccc34)cc2)no1 Linker type: Other Incubation time (hours): 12 Cells: MOLM14, MV4-11 Off-targets reported?: No Comments: IC50 of ligand is 1.6 nM (binding); 1.1-4 (activity). EC50 of ligand is measured on MOLM-14 cell lines Contributed by: Ronen Gabizon MW: 1,176.32 Hbond donors: 5 Hbond acceptors: 19 cLogP: 4.99 TPSA: 295.91 SMILES: show CC(C)(C)c1cc(NC(=O)Nc2ccc(-c3cn4c(n3)sc3cc(OCCN5CCN(C(=O)CCC(=O)NCCCOCCOCCOCCCNC(=O)COc6cccc7c6C(=O)N(C6CCC(=O)NC6=O)C7=O)CC5)ccc34)cc2)no1 Linker type: Other Incubation time (hours): 12 Cells: MOLM14, MV4-11 Off-targets reported?: No Comments: IC50 of ligand is 1.6 nM (binding); 1.1-4 (activity). EC50 of ligand is measured on MOLM-14 cell lines Contributed by: Ronen Gabizon |
Target: Btk Tyrosine-protein kinase BTK P35991 Mus musculus
MW: 931.47 Hbond donors: 5 Hbond acceptors: 16 cLogP: 3.58 TPSA: 233.60 SMILES: show CC(C)S(=O)(=O)c1ccccc1Nc1nc(Nc2ccc(N3CCN(CCOCCOCCNC(=O)CNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)cc2)ncc1Cl Linker type: Other Incubation time (hours): 4 Cells: MOLT-4, MOLM14 IC50: = 10.3 nM DC50: < 100 nM Dmax: > 85 % Off-targets reported?: INCENP, NDUFAB1, CCNH, CCNK, and IKZF1 Comments: General kinase PROTAC, DCmax is for the most degraded kinase. IC50 of the ligand is for 193 kinases in the panel. IC50 of the PROTAC is by FLT3 kinase activity. Contributed by: Ronen Gabizon |
Target: WEE1 Wee1-like protein kinase P30291 Homo sapiens
MW: 931.47 Hbond donors: 5 Hbond acceptors: 16 cLogP: 3.58 TPSA: 233.60 SMILES: show CC(C)S(=O)(=O)c1ccccc1Nc1nc(Nc2ccc(N3CCN(CCOCCOCCNC(=O)CNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)cc2)ncc1Cl Linker type: Other Incubation time (hours): 4 Cells: MOLT-4, MOLM14 IC50: = 10.3 nM DC50: < 100 nM Dmax: > 85 % Off-targets reported?: INCENP, NDUFAB1, CCNH, CCNK, and IKZF1 Comments: General kinase PROTAC, DCmax is for the most degraded kinase. IC50 of the ligand is for 193 kinases in the panel. IC50 of the PROTAC is by FLT3 kinase activity. Contributed by: Ronen Gabizon |
Target: CDK2 Cyclin-dependent kinase 2 P24941 Homo sapiens
MW: 931.47 Hbond donors: 5 Hbond acceptors: 16 cLogP: 3.58 TPSA: 233.60 SMILES: show CC(C)S(=O)(=O)c1ccccc1Nc1nc(Nc2ccc(N3CCN(CCOCCOCCNC(=O)CNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)cc2)ncc1Cl Linker type: Other Incubation time (hours): 4 Cells: MOLT-4, MOLM14 IC50: = 10.3 nM DC50: < 100 nM Dmax: > 85 % Off-targets reported?: INCENP, NDUFAB1, CCNH, CCNK, and IKZF1 Comments: General kinase PROTAC, DCmax is for the most degraded kinase. IC50 of the ligand is for 193 kinases in the panel. IC50 of the PROTAC is by FLT3 kinase activity. Contributed by: Ronen Gabizon |
Target: FER Tyrosine-protein kinase Fer P16591 Homo sapiens
MW: 931.47 Hbond donors: 5 Hbond acceptors: 16 cLogP: 3.58 TPSA: 233.60 SMILES: show CC(C)S(=O)(=O)c1ccccc1Nc1nc(Nc2ccc(N3CCN(CCOCCOCCNC(=O)CNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)cc2)ncc1Cl Linker type: Other Incubation time (hours): 4 Cells: MOLT-4, MOLM14 IC50: = 10.3 nM DC50: < 100 nM Dmax: > 85 % Off-targets reported?: INCENP, NDUFAB1, CCNH, CCNK, and IKZF1 Comments: General kinase PROTAC, DCmax is for the most degraded kinase. IC50 of the ligand is for 193 kinases in the panel. IC50 of the PROTAC is by FLT3 kinase activity. Contributed by: Ronen Gabizon |
Target: CDK4 Cyclin-dependent kinase 4 P11802 Homo sapiens
MW: 931.47 Hbond donors: 5 Hbond acceptors: 16 cLogP: 3.58 TPSA: 233.60 SMILES: show CC(C)S(=O)(=O)c1ccccc1Nc1nc(Nc2ccc(N3CCN(CCOCCOCCNC(=O)CNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)cc2)ncc1Cl Linker type: Other Incubation time (hours): 4 Cells: MOLT-4, MOLM14 IC50: = 10.3 nM DC50: < 100 nM Dmax: > 85 % Off-targets reported?: INCENP, NDUFAB1, CCNH, CCNK, and IKZF1 Comments: General kinase PROTAC, DCmax is for the most degraded kinase. IC50 of the ligand is for 193 kinases in the panel. IC50 of the PROTAC is by FLT3 kinase activity. Contributed by: Ronen Gabizon |
Target: FES Tyrosine-protein kinase Fes/Fps P07332 Homo sapiens
MW: 931.47 Hbond donors: 5 Hbond acceptors: 16 cLogP: 3.58 TPSA: 233.60 SMILES: show CC(C)S(=O)(=O)c1ccccc1Nc1nc(Nc2ccc(N3CCN(CCOCCOCCNC(=O)CNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)cc2)ncc1Cl Linker type: Other Incubation time (hours): 4 Cells: MOLT-4, MOLM14 IC50: = 10.3 nM DC50: < 100 nM Dmax: > 85 % Off-targets reported?: INCENP, NDUFAB1, CCNH, CCNK, and IKZF1 Comments: General kinase PROTAC, DCmax is for the most degraded kinase. IC50 of the ligand is for 193 kinases in the panel. IC50 of the PROTAC is by FLT3 kinase activity. Contributed by: Ronen Gabizon |
Target: LCK Tyrosine-protein kinase Lck P06239 Homo sapiens
MW: 931.47 Hbond donors: 5 Hbond acceptors: 16 cLogP: 3.58 TPSA: 233.60 SMILES: show CC(C)S(=O)(=O)c1ccccc1Nc1nc(Nc2ccc(N3CCN(CCOCCOCCNC(=O)CNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)cc2)ncc1Cl Linker type: Other Incubation time (hours): 4 Cells: MOLT-4, MOLM14 IC50: = 10.3 nM DC50: < 100 nM Dmax: > 85 % Off-targets reported?: INCENP, NDUFAB1, CCNH, CCNK, and IKZF1 Comments: General kinase PROTAC, DCmax is for the most degraded kinase. IC50 of the ligand is for 193 kinases in the panel. IC50 of the PROTAC is by FLT3 kinase activity. Contributed by: Ronen Gabizon |
Target: ULK1 Serine/threonine-protein kinase ULK1 O75385 Homo sapiens
MW: 931.47 Hbond donors: 5 Hbond acceptors: 16 cLogP: 3.58 TPSA: 233.60 SMILES: show CC(C)S(=O)(=O)c1ccccc1Nc1nc(Nc2ccc(N3CCN(CCOCCOCCNC(=O)CNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)cc2)ncc1Cl Linker type: Other Incubation time (hours): 4 Cells: MOLT-4, MOLM14 IC50: = 10.3 nM DC50: < 100 nM Dmax: > 85 % Off-targets reported?: INCENP, NDUFAB1, CCNH, CCNK, and IKZF1 Comments: General kinase PROTAC, DCmax is for the most degraded kinase. IC50 of the ligand is for 193 kinases in the panel. IC50 of the PROTAC is by FLT3 kinase activity. Contributed by: Ronen Gabizon |
Target: GAK Cyclin-G-associated kinase O14976 Homo sapiens
MW: 931.47 Hbond donors: 5 Hbond acceptors: 16 cLogP: 3.58 TPSA: 233.60 SMILES: show CC(C)S(=O)(=O)c1ccccc1Nc1nc(Nc2ccc(N3CCN(CCOCCOCCNC(=O)CNc4cccc5c4C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)cc2)ncc1Cl Linker type: Other Incubation time (hours): 4 Cells: MOLT-4, MOLM14 IC50: = 10.3 nM DC50: < 100 nM Dmax: > 85 % Off-targets reported?: INCENP, NDUFAB1, CCNH, CCNK, and IKZF1 Comments: General kinase PROTAC, DCmax is for the most degraded kinase. IC50 of the ligand is for 193 kinases in the panel. IC50 of the PROTAC is by FLT3 kinase activity. Contributed by: Ronen Gabizon |