ChEMBL ligand: CHEMBL4128069
protein kinase AMP-activated catalytic subunit alpha 2/5`-AMP-activated protein kinase catalytic subunit alpha-2 in Human [ChEMBL: CHEMBL2116] [GtoPdb: 1542] [UniProtKB: P54646] There should be some charts here, you may need to enable JavaScript!
unc-51 like autophagy activating kinase 1/Serine/threonine-protein kinase ULK1 in Human [ChEMBL: CHEMBL6006] [GtoPdb: 2271] [UniProtKB: O75385] 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!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
protein kinase AMP-activated catalytic subunit alpha 2/5`-AMP-activated protein kinase catalytic subunit alpha-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2116] [GtoPdb: 1542] [UniProtKB: P54646]
ChEMBL	Inhibition of human AMPK	B	6.97	pIC50	108	nM	IC50	Eur J Med Chem (2024) 267: 116117-116117 [PMID:38295689]
unc-51 like autophagy activating kinase 1/Serine/threonine-protein kinase ULK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6006] [GtoPdb: 2271] [UniProtKB: O75385]
ChEMBL	Inhibition of ULK1 (unknown origin) expressed in HEK293T cells incubated for 2 hrs by NanoBRET assay	B	6.11	pIC50	785	nM	IC50	J Med Chem (2020) 63: 14609-14625 [PMID:33200929]
ChEMBL	ULK1 inhibition assay: ULK1 inhibition assay is a screening assay to identify compounds that inhibit kinase activity of ULK1 using the ULKtide peptide. In some embodiments, the method contacting a candidate compound, ULK1 and a recombinant ULKtide peptide (or variant thereof); detecting phosphorylation of the recombinant peptide in the presence and absence of the candidate compound; and identifying a compound that inhibits kinase activity of ULK1 if phosphorylation of the recombinant peptide is decreased in the presence of the candidate compound compared to in the absence of the candidate compound.	B	6.7	pIC50	<200	nM	IC50	US-10774092-B2. ULK1 inhibitors and methods using same (2020)
ChEMBL	ULK1 inhibition assay: Gamma-32P assays to measure ULK1 kinase activity were performed as previously described. Briefly, Flag ULK1 was transfected into HEK293T cells and 20 hours later treated as indicated. The immmunoprecipitate was washed in IP buffer 3 times, and washed in kinase buffer (25 mM MOPS, pH 7.5, 1 mM EGTA, 0.1 mM Na3VO4, 15 mM MgCl2,). Hot and cold ATP were added at a 100 μM final concentration. As substrates, GST or the recombinant protein GST-Atg101 purified from E. coli were used at 1 μg for each reaction. Reactions were boiled, run out on SDS page gel. The gel was dried, and imaged using PhosphoImager software. For cold assays to asses ULK1, Flag ULK1 which was transiently overexpressed and immunoprecipited from HEK293T cells. Reactions were then run out on SDS page gel, transferred to PVDF membrane and blotted for total levelsFluorescence MicroscopyVps34flox/flox MEFs were reconstituted with Flag-VPS34 and either p40FX or GFP-DFCP1. 48 hours post infection with adenovirus expressing Cre recombinase (MOI of 100), cells were plated on glass coverslips at a density of 3×105 cells per well in 6-well tissue culture plates. 18 h later, cells were fixed in 4% PFA in PBS for 10 minutes and permeabilized in 0.2% Triton in PBS for 10 minutes. The following primary antibodies were used: mouse anti-Myc epitope and LC3B XP antibody (2276 and 3868 respectively, Cell Signaling Technologies). Secondary antibodies were anti-rabbit Alexa488 and anti-mouse Alexa594 (Molecular Probes, 1:1000. Cells were then fixed and counter stained with DAPI. Coverslips were mounted in FluoromountG (SouthernBiothech). Images were acquired on a Zeiss Axioplan2 epifluorescence microscope coupled to the Openlab software. Confocal images of mitotracker were taken on Zeiss LSM 710 laser scanning confocal microscope. 10 random fields per condition were acquired using the 100× objective and representative images shown. Glass coverslips were mounted directly on plate with FluoromountG and images taken on Zeiss Axioplan2 epifluorescence microscope.	B	6.7	pIC50	<200	nM	IC50	US-10266549-B2. ULK1 inhibitors and methods using same (2019)
ChEMBL	ULK1 inhibition assay: Gamma-32P assays to measure ULK1 kinase activity were performed as previously described. Briefly, Flag ULK1 was transfected into HEK293T cells and 20 hours later treated as indicated. The immmunoprecipitate was washed in IP buffer 3 times, and washed in kinase buffer (25 mM MOPS, pH 7.5, 1 mM EGTA, 0.1 mM Na3VO4, 15 mM MgCl2,). Hot and cold ATP were added at a 100 μM final concentration. As substrates, GST or the recombinant protein GST-Atg101 purified from E. coli were used at 1 μg for each reaction. Reactions were boiled, run out on SDS page gel. The gel was dried, and imaged using PhosphoImager software. For cold assays to asses ULK1, Flag ULK1 which was transiently overexpressed and immunoprecipited from HEK293T cells. Reactions were then run out on SDS page gel, transferred to PVDF membrane and blotted for total levelsFluorescence MicroscopyVps34flox/flox MEFs were reconstituted with Flag-VPS34 and either p40FX or GFP-DFCP1. 48 hours post infection with adenovirus expressing Cre recombinase (MOI of 100), cells were plated on glass coverslips at a density of 3×105 cells per well in 6-well tissue culture plates. 18 h later, cells were fixed in 4% PFA in PBS for 10 minutes and permeabilized in 0.2% Triton in PBS for 10 minutes. The following primary antibodies were used: mouse anti-Myc epitope and LC3B XP antibody (2276 and 3868 respectively, Cell Signaling Technologies). Secondary antibodies were anti-rabbit Alexa488 and anti-mouse Alexa594 (Molecular Probes, 1:1000. Cells were then fixed and counter stained with DAPI. Coverslips were mounted in FluoromountG (SouthernBiothech). Images were acquired on a Zeiss Axioplan2 epifluorescence microscope coupled to the Openlab software. Confocal images of mitotracker were taken on Zeiss LSM 710 laser scanning confocal microscope. 10 random fields per condition were acquired using the 100× objective and representative images shown. Glass coverslips were mounted directly on plate with FluoromountG and images taken on Zeiss Axioplan2 epifluorescence microscope.	B	6.7	pIC50	<200	nM	IC50	US-10266549-B2. ULK1 inhibitors and methods using same (2019)
ChEMBL	Inhibition of recombinant human ULK1 (1-649) expressed in Sf9 cells using myelin basic protein as substrate by ADP-glo assay	B	6.89	pIC50	130	nM	IC50	J Med Chem (2020) 63: 14609-14625 [PMID:33200929]
GtoPdb	-	-	6.89	pIC50	130	nM	IC50	Mol Cell (2015) 59: 285-97 [PMID:26118643]
ChEMBL	Competitive inhibition of ULK1 (unknown origin) in presence of ATP	B	6.97	pIC50	108	nM	IC50	Eur J Med Chem (2022) 244: 114846-114846 [PMID:36283182]
ChEMBL	Inhibition of FLAG-tagged ULK1 (unknown origin) expressed in HEK293T cells using GST-labelled Atg101 as substrate in presence of gamma-[32]P-ATP	B	6.97	pIC50	108	nM	IC50	J Med Chem (2018) 61: 4656-4687 [PMID:29211480]
ChEMBL	Inhibition of ULK1 (unknown origin) by 32P-ATP radio active assay	B	6.97	pIC50	108	nM	IC50	Eur J Med Chem (2020) 208: 112782-112782 [PMID:32961380]
ChEMBL	Inhibition of GST-tagged ULK1 (unknown origin)	B	6.97	pIC50	108	nM	IC50	J Med Chem (2018) 61: 6491-6500 [PMID:29509411]
ChEMBL	Inhibition of ULK1 (unknown origin)	B	6.97	pIC50	108	nM	IC50	Eur J Med Chem (2024) 268: 116273-116273 [PMID:38432059]
ChEMBL	Inhibition of human ULK1	B	7.42	pIC50	38	nM	IC50	iScience (2018) 8: 74-84 [PMID:30292171]
ChEMBL	Inhibition of ULK1 phosphorylation at Ser15 residue in HEK293 cells incubated for 1 hr by chemiluminescence based immunoblotting analysis	B	5.62	pEC50	2400	nM	EC50	iScience (2018) 8: 74-84 [PMID:30292171]
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	Inhibition of ULK2 (unknown origin) expressed in HEK293T cells incubated for 2 hrs by NanoBRET assay	B	5.34	pIC50	4578	nM	IC50	J Med Chem (2020) 63: 14609-14625 [PMID:33200929]
ChEMBL	Inhibition of recombinant human ULK2 (1 to 478 residues) expressed in Sf9 cells using myelin basic protein as substrate by ADP-glo assay	B	5.61	pIC50	2448	nM	IC50	J Med Chem (2020) 63: 14609-14625 [PMID:33200929]
ChEMBL	Inhibition of GST-tagged ULK2 (unknown origin)	B	6.15	pIC50	711	nM	IC50	J Med Chem (2018) 61: 6491-6500 [PMID:29509411]
ChEMBL	Inhibition of ULK2 (unknown origin)	B	6.15	pIC50	711	nM	IC50	Eur J Med Chem (2020) 208: 112782-112782 [PMID:32961380]
ChEMBL	Inhibition of ULK2 (unknown origin)	B	6.15	pIC50	711	nM	IC50	Eur J Med Chem (2024) 268: 116273-116273 [PMID:38432059]
ChEMBL	Inhibition of human ULK2	B	6.67	pIC50	212	nM	IC50	iScience (2018) 8: 74-84 [PMID:30292171]
ChEMBL	Inhibition of ULK2 (unknown origin)	B	7.96	pIC50	11	nM	IC50	J Med Chem (2018) 61: 4656-4687 [PMID:29211480]

ChEMBL data shown on this page come from version 36:

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]