ChEMBL ligand: CHEMBL3904602 (G1t38, G1T-38, G1T38, G1T38 FREE BASE, Lerociclib)
cyclin dependent kinase 6/CDK6/cyclin D3 in Human [ChEMBL: CHEMBL2111448] [GtoPdb: 1978] [UniProtKB: P30281, Q00534] There should be some charts here, you may need to enable JavaScript!
cyclin dependent kinase 9/CDK9/Cyclin-H in Human [ChEMBL: CHEMBL4523632] [GtoPdb: 1981] [UniProtKB: P50750, P51946] There should be some charts here, you may need to enable JavaScript!
cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941] There should be some charts here, you may need to enable JavaScript!
cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin E1 in Human [ChEMBL: CHEMBL1907605] [GtoPdb: 1973] [UniProtKB: P24864, P24941] There should be some charts here, you may need to enable JavaScript!
cyclin dependent kinase 4/Cyclin-dependent kinase 4 in Human [ChEMBL: CHEMBL331] [GtoPdb: 1976] [UniProtKB: P11802] There should be some charts here, you may need to enable JavaScript!
cyclin dependent kinase 4/Cyclin-dependent kinase 4/cyclin D1 in Human [ChEMBL: CHEMBL1907601] [GtoPdb: 1976] [UniProtKB: P11802, P24385] There should be some charts here, you may need to enable JavaScript!
cyclin dependent kinase 6/Cyclin-dependent kinase 6 in Human [ChEMBL: CHEMBL2508] [GtoPdb: 1978] [UniProtKB: Q00534] There should be some charts here, you may need to enable JavaScript!
cyclin dependent kinase 9/Cyclin-dependent kinase 9 in Human [ChEMBL: CHEMBL3116] [GtoPdb: 1981] [UniProtKB: P50750] There should be some charts here, you may need to enable JavaScript!
TTK protein kinase/Dual specificity protein kinase TTK in Human [ChEMBL: CHEMBL3983] [GtoPdb: 2264] [UniProtKB: P33981] There should be some charts here, you may need to enable JavaScript!
NUAK family, SNF1-like kinase, 2/NUAK family SNF1-like kinase 2 in Human [ChEMBL: CHEMBL5698] [GtoPdb: 2130] [UniProtKB: Q9H093] There should be some charts here, you may need to enable JavaScript!
NIMA related kinase 10/Serine/threonine-protein kinase Nek10 in Human [ChEMBL: CHEMBL3108655] [GtoPdb: 2115] [UniProtKB: Q6ZWH5] There should be some charts here, you may need to enable JavaScript!
unc-51 like autophagy activating kinase 2/Serine/threonine-protein kinase ULK2 in Human [ChEMBL: CHEMBL5435] [GtoPdb: 2272] [UniProtKB: Q8IYT8] There should be some charts here, you may need to enable JavaScript!
fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888] 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 6/CDK6/cyclin D3 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111448] [GtoPdb: 1978] [UniProtKB: P30281, Q00534]
ChEMBL	Caliper Assay: Selected compounds disclosed herein were tested in CDK4/cyclinD1, CDK6/CycD3 CDK2/CycA and CDK2/cyclinE kinase assays by Nanosyn (Santa Clara, Calif.) to determine their inhibitory effect on these CDKs. The assays were performed using microfluidic kinase detection technology (Caliper Assay Platform). The compounds were tested in 12-point dose-response format in singlicate at Km for ATP. Phosphoacceptor substrate peptide concentration used was 1 μM for all assays and Staurosporine was used as the reference compound for all assays. Specifics of each assay are as described below:CDK2/CyclinA: Enzyme concentration: 0.2 nM; ATP concentration: 50 μM; Incubation time: 3 hr.CDK2/CyclinE: Enzyme concentration: 0.28 nM; ATP concentration: 100 μM; Incubation time: 1 hr.CDK4/CyclinD1: Enzyme concentration: 1 nM; ATP concentration: 200 μM; Incubation time: 10 hr.CDK6/CyclinD3: Enzyme concentration: 1 nM; ATP concentration: 300 μM; Incubation time: 3 hr.	B	8.33	pIC50	4.7	nM	IC50	US-9464092-B2. Transient protection of normal cells during chemotherapy (2016)
GtoPdb	Inhibition of CDK6/cyclin D3 complex	-	8.33	pIC50	4.7	nM	IC50	US9464092B2. Transient protection of normal cells during chemotherapy (2016)
cyclin dependent kinase 9/CDK9/Cyclin-H in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4523632] [GtoPdb: 1981] [UniProtKB: P50750, P51946]
ChEMBL	Inhibition of CDK9/cyclin H (unknown origin)	B	6.55	pIC50	280	nM	IC50	Bioorg Med Chem Lett (2019) 29: 126637-126637 [PMID:31477350]
cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
ChEMBL	Caliper Assay: Selected compounds disclosed herein were tested in CDK4/cyclinD1, CDK6/CycD3 CDK2/CycA and CDK2/cyclinE kinase assays by Nanosyn (Santa Clara, Calif.) to determine their inhibitory effect on these CDKs. The assays were performed using microfluidic kinase detection technology (Caliper Assay Platform). The compounds were tested in 12-point dose-response format in singlicate at Km for ATP. Phosphoacceptor substrate peptide concentration used was 1 μM for all assays and Staurosporine was used as the reference compound for all assays. Specifics of each assay are as described below:CDK2/CyclinA: Enzyme concentration: 0.2 nM; ATP concentration: 50 μM; Incubation time: 3 hr.CDK2/CyclinE: Enzyme concentration: 0.28 nM; ATP concentration: 100 μM; Incubation time: 1 hr.CDK4/CyclinD1: Enzyme concentration: 1 nM; ATP concentration: 200 μM; Incubation time: 10 hr.CDK6/CyclinD3: Enzyme concentration: 1 nM; ATP concentration: 300 μM; Incubation time: 3 hr.	B	5.45	pIC50	3580	nM	IC50	US-9464092-B2. Transient protection of normal cells during chemotherapy (2016)
ChEMBL	Caliper Assay: Selected compounds disclosed herein were tested in CDK4/cyclinD1, CDK6/CycD3 CDK2/CycA and CDK2/cyclinE kinase assays by Nanosyn (Santa Clara, Calif.) to determine their inhibitory effect on these CDKs. The assays were performed using microfluidic kinase detection technology (Caliper Assay Platform). The compounds were tested in 12-point dose-response format in singlicate at Km for ATP. Phosphoacceptor substrate peptide concentration used was 1 μM for all assays and Staurosporine was used as the reference compound for all assays. Specifics of each assay are as described below:CDK2/CyclinA: Enzyme concentration: 0.2 nM; ATP concentration: 50 μM; Incubation time: 3 hr.CDK2/CyclinE: Enzyme concentration: 0.28 nM; ATP concentration: 100 μM; Incubation time: 1 hr.CDK4/CyclinD1: Enzyme concentration: 1 nM; ATP concentration: 200 μM; Incubation time: 10 hr.CDK6/CyclinD3: Enzyme concentration: 1 nM; ATP concentration: 300 μM; Incubation time: 3 hr.	B	5.82	pIC50	1510	nM	IC50	US-9464092-B2. Transient protection of normal cells during chemotherapy (2016)
ChEMBL	Caliper Assay: Selected compounds disclosed herein were tested in CDK4/cyclinD1, CDK6/CycD3 CDK2/CycA and CDK2/cyclinE kinase assays by Nanosyn (Santa Clara, Calif.) to determine their inhibitory effect on these CDKs. The assays were performed using microfluidic kinase detection technology (Caliper Assay Platform). The compounds were tested in 12-point dose-response format in singlicate at Km for ATP. Phosphoacceptor substrate peptide concentration used was 1 μM for all assays and Staurosporine was used as the reference compound for all assays. Specifics of each assay are as described below:CDK2/CyclinA: Enzyme concentration: 0.2 nM; ATP concentration: 50 μM; Incubation time: 3 hr.CDK2/CyclinE: Enzyme concentration: 0.28 nM; ATP concentration: 100 μM; Incubation time: 1 hr.CDK4/CyclinD1: Enzyme concentration: 1 nM; ATP concentration: 200 μM; Incubation time: 10 hr.CDK6/CyclinD3: Enzyme concentration: 1 nM; ATP concentration: 300 μM; Incubation time: 3 hr.	B	8.45	pIC50	3.58	nM	IC50	US-9464092-B2. Transient protection of normal cells during chemotherapy (2016)
ChEMBL	Caliper Assay: Selected compounds disclosed herein were tested in CDK4/cyclinD1, CDK6/CycD3 CDK2/CycA and CDK2/cyclinE kinase assays by Nanosyn (Santa Clara, Calif.) to determine their inhibitory effect on these CDKs. The assays were performed using microfluidic kinase detection technology (Caliper Assay Platform). The compounds were tested in 12-point dose-response format in singlicate at Km for ATP. Phosphoacceptor substrate peptide concentration used was 1 μM for all assays and Staurosporine was used as the reference compound for all assays. Specifics of each assay are as described below:CDK2/CyclinA: Enzyme concentration: 0.2 nM; ATP concentration: 50 μM; Incubation time: 3 hr.CDK2/CyclinE: Enzyme concentration: 0.28 nM; ATP concentration: 100 μM; Incubation time: 1 hr.CDK4/CyclinD1: Enzyme concentration: 1 nM; ATP concentration: 200 μM; Incubation time: 10 hr.CDK6/CyclinD3: Enzyme concentration: 1 nM; ATP concentration: 300 μM; Incubation time: 3 hr.	B	8.82	pIC50	1.51	nM	IC50	US-9464092-B2. Transient protection of normal cells during chemotherapy (2016)
cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin E1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907605] [GtoPdb: 1973] [UniProtKB: P24864, P24941]
ChEMBL	Inhibition of human CDK2/cyclin E	B	7	pEC50	<100	nM	EC50	Bioorg Med Chem Lett (2019) 29: 126637-126637 [PMID:31477350]
cyclin dependent kinase 4/Cyclin-dependent kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL331] [GtoPdb: 1976] [UniProtKB: P11802]
GtoPdb	Inhibition of CDK4/cyclin D1	-	9	pIC50	1	nM	IC50	US9464092B2. Transient protection of normal cells during chemotherapy (2016)
ChEMBL	Inhibition of CDK4 (unknown origin)	B	9	pIC50	1	nM	IC50	Eur J Med Chem (2020) 203: 112571-112571 [PMID:32707525]
cyclin dependent kinase 4/Cyclin-dependent kinase 4/cyclin D1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907601] [GtoPdb: 1976] [UniProtKB: P11802, P24385]
ChEMBL	Caliper Assay: Selected compounds disclosed herein were tested in CDK4/cyclinD1, CDK6/CycD3 CDK2/CycA and CDK2/cyclinE kinase assays by Nanosyn (Santa Clara, Calif.) to determine their inhibitory effect on these CDKs. The assays were performed using microfluidic kinase detection technology (Caliper Assay Platform). The compounds were tested in 12-point dose-response format in singlicate at Km for ATP. Phosphoacceptor substrate peptide concentration used was 1 μM for all assays and Staurosporine was used as the reference compound for all assays. Specifics of each assay are as described below:CDK2/CyclinA: Enzyme concentration: 0.2 nM; ATP concentration: 50 μM; Incubation time: 3 hr.CDK2/CyclinE: Enzyme concentration: 0.28 nM; ATP concentration: 100 μM; Incubation time: 1 hr.CDK4/CyclinD1: Enzyme concentration: 1 nM; ATP concentration: 200 μM; Incubation time: 10 hr.CDK6/CyclinD3: Enzyme concentration: 1 nM; ATP concentration: 300 μM; Incubation time: 3 hr.	B	8.97	pIC50	1.06	nM	IC50	US-9464092-B2. Transient protection of normal cells during chemotherapy (2016)
GtoPdb	Inhibition of CDK4/cyclin D1	-	9	pIC50	1	nM	IC50	US9464092B2. Transient protection of normal cells during chemotherapy (2016)
ChEMBL	Caliper Assay: Selected compounds disclosed herein were tested in CDK4/cyclinD1, CDK6/CycD3 CDK2/CycA and CDK2/cyclinE kinase assays by Nanosyn (Santa Clara, Calif.) to determine their inhibitory effect on these CDKs. The assays were performed using microfluidic kinase detection technology (Caliper Assay Platform). The compounds were tested in 12-point dose-response format in singlicate at Km for ATP. Phosphoacceptor substrate peptide concentration used was 1 μM for all assays and Staurosporine was used as the reference compound for all assays. Specifics of each assay are as described below:CDK2/CyclinA: Enzyme concentration: 0.2 nM; ATP concentration: 50 μM; Incubation time: 3 hr.CDK2/CyclinE: Enzyme concentration: 0.28 nM; ATP concentration: 100 μM; Incubation time: 1 hr.CDK4/CyclinD1: Enzyme concentration: 1 nM; ATP concentration: 200 μM; Incubation time: 10 hr.CDK6/CyclinD3: Enzyme concentration: 1 nM; ATP concentration: 300 μM; Incubation time: 3 hr.	B	9	pIC50	1	nM	IC50	US-9464092-B2. Transient protection of normal cells during chemotherapy (2016)
ChEMBL	Inhibition of human CDK4/cyclinD1	B	7	pEC50	<100	nM	EC50	Bioorg Med Chem Lett (2019) 29: 126637-126637 [PMID:31477350]
cyclin dependent kinase 6/Cyclin-dependent kinase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2508] [GtoPdb: 1978] [UniProtKB: Q00534]
GtoPdb	Inhibition of CDK6/cyclin D3 complex	-	8.33	pIC50	4.7	nM	IC50	US9464092B2. Transient protection of normal cells during chemotherapy (2016)
ChEMBL	Inhibition of CDK6 (unknown origin)	B	8.7	pIC50	2	nM	IC50	Eur J Med Chem (2020) 203: 112571-112571 [PMID:32707525]
cyclin dependent kinase 9/Cyclin-dependent kinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3116] [GtoPdb: 1981] [UniProtKB: P50750]
ChEMBL	Inhibition of CDK9 (unknown origin)	B	7.55	pIC50	28	nM	IC50	Eur J Med Chem (2020) 203: 112571-112571 [PMID:32707525]
TTK protein kinase/Dual specificity protein kinase TTK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3983] [GtoPdb: 2264] [UniProtKB: P33981]
ChEMBL	Binding affinity to TTK (unknown origin)	B	8.38	pKd	4.2	nM	Kd	Bioorg Med Chem Lett (2019) 29: 126637-126637 [PMID:31477350]
NUAK family, SNF1-like kinase, 2/NUAK family SNF1-like kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5698] [GtoPdb: 2130] [UniProtKB: Q9H093]
ChEMBL	Binding affinity to SNARK (unknown origin)	B	9.15	pKd	0.7	nM	Kd	Bioorg Med Chem Lett (2019) 29: 126637-126637 [PMID:31477350]
NIMA related kinase 10/Serine/threonine-protein kinase Nek10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3108655] [GtoPdb: 2115] [UniProtKB: Q6ZWH5]
ChEMBL	Binding affinity to NEK10 (unknown origin)	B	9.7	pKd	0.2	nM	Kd	Bioorg Med Chem Lett (2019) 29: 126637-126637 [PMID:31477350]
unc-51 like autophagy activating kinase 2/Serine/threonine-protein kinase ULK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5435] [GtoPdb: 2272] [UniProtKB: Q8IYT8]
ChEMBL	Binding affinity to ULK2 (unknown origin)	B	8.26	pKd	5.5	nM	Kd	Bioorg Med Chem Lett (2019) 29: 126637-126637 [PMID:31477350]
fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
ChEMBL	Binding affinity to human FLT3 D835V mutant	B	7.66	pKd	22	nM	Kd	Bioorg Med Chem Lett (2019) 29: 126637-126637 [PMID:31477350]
ChEMBL	Binding affinity to human FLT3 ITD mutant	B	8.19	pKd	6.5	nM	Kd	Bioorg Med Chem Lett (2019) 29: 126637-126637 [PMID:31477350]

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]