Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
ChEMBL ligand: CHEMBL1944698 (TG02, SB-1317, SB1317, EX45, Zotiraciclib, Tg-02, Tg02) |
---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
---|---|---|---|---|---|---|---|---|
cyclin dependent kinase 3/CDK3/Cyclin E in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038471] [GtoPdb: 1975] [UniProtKB: P24864, Q00526] | ||||||||
ChEMBL | Inhibition of recombinant human full-length C-terminal His6-tagged CDK3/full-length human N-terminal GST-tagged Cyclin E expressed in baculovirus infected Sf21 insect cells using histone H1 as substrate | B | 8.1 | pIC50 | 8 | nM | IC50 | J Med Chem (2019) 62: 4233-4251 [PMID:30543440] |
GtoPdb | - | - | 8.1 | pIC50 | 8 | nM | IC50 | Leukemia (2012) 26: 236-43 [PMID:21860433] |
ChEMBL | Inhibition of recombinant human full length C-terminal His6-tagged CDK3/N-terminal GST-tagged cyclin E expressed in baculovirus infected Sf21 insect cells using Histone H1 as substrate | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2016) 59: 8667-8684 [PMID:27171036] |
cyclin dependent kinase 7/CDK7/Cyclin H/MNAT1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038473] [GtoPdb: 1979] [UniProtKB: P50613, P51946, P51948] | ||||||||
ChEMBL | Inhibition of recombinant human C-terminal His6-tagged full length CDK7/untagged recombinant full length human Cyclin H/N-terminal GST-tagged recombinant full length human MAT1 expressed in baculovirus infected Sf21 insect cells using cdk7 peptide as substrate | B | 7.43 | pIC50 | 37 | nM | IC50 | J Med Chem (2019) 62: 4233-4251 [PMID:30543440] |
ChEMBL | Inhibition of recombinant human full length C-terminal His6-tagged CDK7/cyclin H/N-terminal GST-tagged MAT1 expressed in baculovirus infected Sf21 insect cells using cdk7 substrate peptide | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2016) 59: 8667-8684 [PMID:27171036] |
cyclin dependent kinase 9/CDK9/Cyclin K in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038475] [GtoPdb: 1981] [UniProtKB: O75909, P50750] | ||||||||
GtoPdb | - | - | 8.52 | pIC50 | 3 | nM | IC50 | Leukemia (2012) 26: 236-43 [PMID:21860433] |
ChEMBL | Inhibition of human recombinant full length His-tagged CDK9/cyclin K expressed in baculovirus expression system | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2019) 62: 4233-4251 [PMID:30543440] |
cyclin dependent kinase 1/Cyclin-dependent kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL308] [GtoPdb: 1961] [UniProtKB: P06493] | ||||||||
GtoPdb | - | - | 8.05 | pIC50 | 9 | nM | IC50 | Leukemia (2012) 26: 236-43 [PMID:21860433] |
ChEMBL | Inhibition of CDK1 (unknown origin) | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2016) 59: 8667-8684 [PMID:27171036] |
cyclin dependent kinase 1/Cyclin-dependent kinase 1/cyclin B1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907602] [GtoPdb: 1961] [UniProtKB: P06493, P14635] | ||||||||
ChEMBL | Inhibition of human recombinant full-length His-tagged CDK1/cyclin B1 expressed in baculovirus expression system | B | 8.05 | pIC50 | 9 | nM | IC50 | J Med Chem (2019) 62: 4233-4251 [PMID:30543440] |
GtoPdb | - | - | 8.05 | pIC50 | 9 | nM | IC50 | Leukemia (2012) 26: 236-43 [PMID:21860433] |
cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941] | ||||||||
ChEMBL | Inhibition of CDK2 in human MV411 cells assessed as Rb phosphorylation after 24 hrs by Western blot analysis | B | 6.89 | pIC50 | 130 | nM | IC50 | J. Med. Chem. (2012) 55: 169-196 [PMID:22148278] |
GtoPdb | - | - | 8.3 | pIC50 | 5 | nM | IC50 |
J Med Chem (2012) 55: 169-96 [PMID:22148278]; Leukemia (2012) 26: 236-43 [PMID:21860433] |
ChEMBL | Inhibition of CDK2 (unknown origin) | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2016) 59: 8667-8684 [PMID:27171036] |
cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin A in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094128] [GtoPdb: 1973] [UniProtKB: P20248, P24941, P78396] | ||||||||
ChEMBL | Inhibition of recombinant Cdk2/cyclin A using RbING as substrate after 2 hrs by luminescence assay | B | 7.89 | pIC50 | 13 | nM | IC50 | J. Med. Chem. (2012) 55: 169-196 [PMID:22148278] |
GtoPdb | - | - | 8.3 | pIC50 | 5 | nM | IC50 |
J Med Chem (2012) 55: 169-96 [PMID:22148278]; Leukemia (2012) 26: 236-43 [PMID:21860433] |
cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin E1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907605] [GtoPdb: 1973] [UniProtKB: P24864, P24941] | ||||||||
GtoPdb | - | - | 8.3 | pIC50 | 5 | nM | IC50 |
J Med Chem (2012) 55: 169-96 [PMID:22148278]; Leukemia (2012) 26: 236-43 [PMID:21860433] |
ChEMBL | Inhibition of human recombinant GST-tagged CDK2/cyclin E1 | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2019) 62: 4233-4251 [PMID:30543440] |
cyclin dependent kinase 5/Cyclin-dependent kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4036] [GtoPdb: 1977] [UniProtKB: Q00535] | ||||||||
GtoPdb | - | - | 8.4 | pIC50 | 4 | nM | IC50 | Leukemia (2012) 26: 236-43 [PMID:21860433] |
ChEMBL | Inhibition of human GST-tagged CDK5 | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2016) 59: 8667-8684 [PMID:27171036] |
cyclin dependent kinase 5/Cyclin-dependent kinase 5/CDK5 activator 1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907600] [GtoPdb: 1977] [UniProtKB: Q00535, Q15078] | ||||||||
ChEMBL | Inhibition of human recombinant full-length GST/His-tagged CDK5/p25 expressed in baculovirus expression system by Z'-Lyte assay | B | 8.4 | pIC50 | 4 | nM | IC50 | J Med Chem (2019) 62: 4233-4251 [PMID:30543440] |
GtoPdb | - | - | 8.4 | pIC50 | 4 | nM | IC50 | Leukemia (2012) 26: 236-43 [PMID:21860433] |
cyclin dependent kinase 6/Cyclin-dependent kinase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2508] [GtoPdb: 1978] [UniProtKB: Q00534] | ||||||||
ChEMBL | Inhibition of human CDK6 | B | 7 | pIC50 | >100 | nM | IC50 | J Med Chem (2019) 62: 4233-4251 [PMID:30543440] |
cyclin dependent kinase 9/Cyclin-dependent kinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3116] [GtoPdb: 1981] [UniProtKB: P50750] | ||||||||
GtoPdb | - | - | 8.52 | pIC50 | 3 | nM | IC50 | Leukemia (2012) 26: 236-43 [PMID:21860433] |
ChEMBL | Inhibition of human GST-tagged CDK9 | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2016) 59: 8667-8684 [PMID:27171036] |
Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674] | ||||||||
ChEMBL | Inhibition of human recombinant JAK2 using Z'LYTETry6 peptide substrate after 1 hr by microplate reader | B | 6.77 | pIC50 | 170 | nM | IC50 | Eur. J. Med. Chem. (2015) 95: 104-115 [PMID:25800646] |
ChEMBL | Inhibition of recombinant JAK2 using poly(Glu,Ala,Tyr) as substrate after 2 hrs by luminescence assay | B | 7.14 | pIC50 | 73 | nM | IC50 | J. Med. Chem. (2012) 55: 169-196 [PMID:22148278] |
ChEMBL | Inhibition of human recombinant GST-tagged JAK2 expressed in baculovirus expression system | B | 7.14 | pIC50 | 73 | nM | IC50 | J Med Chem (2016) 59: 8667-8684 [PMID:27171036] |
GtoPdb | - | - | 7.72 | pIC50 | 19 | nM | IC50 |
J Med Chem (2012) 55: 169-96 [PMID:22148278]; Leukemia (2012) 26: 236-43 [PMID:21860433] |
fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888] | ||||||||
ChEMBL | Inhibition of recombinant Flt3 using poly(Glu,Tyr) as substrate after 2 hrs by luminescence assay | B | 7.25 | pIC50 | 56 | nM | IC50 | J. Med. Chem. (2012) 55: 169-196 [PMID:22148278] |
ChEMBL | Inhibition of human recombinant FLT3 after 1 hr by LanthaScreen assay platform | B | 7.38 | pIC50 | 42 | nM | IC50 | Eur. J. Med. Chem. (2015) 95: 104-115 [PMID:25800646] |
ChEMBL | Inhibition of human recombinant N-terminal GST-tagged FLT3 D835Y mutant expressed in baculovirus infected Sf21 insect cells using abltide as substrate | B | 7.68 | pIC50 | 21 | nM | IC50 | J Med Chem (2016) 59: 8667-8684 [PMID:27171036] |
GtoPdb | - | - | 7.72 | pIC50 | 19 | nM | IC50 |
J Med Chem (2012) 55: 169-96 [PMID:22148278]; Leukemia (2012) 26: 236-43 [PMID:21860433] |
colony stimulating factor 1 receptor in Human [GtoPdb: 1806] [UniProtKB: P07333] | ||||||||
GtoPdb | - | - | 7.57 | pIC50 | 27 | nM | IC50 | Leukemia (2012) 26: 236-43 [PMID:21860433] |
Janus kinase 1 in Human [GtoPdb: 2047] [UniProtKB: P23458] | ||||||||
GtoPdb | - | - | 7.23 | pIC50 | 59 | nM | IC50 | Leukemia (2012) 26: 236-43 [PMID:21860433] |
tyrosine kinase 2 in Human [GtoPdb: 2269] [UniProtKB: P29597] | ||||||||
GtoPdb | - | - | 7.85 | pIC50 | 14 | nM | IC50 | Leukemia (2012) 26: 236-43 [PMID:21860433] |
ChEMBL data shown on this page come from version 28:
Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]