curcumin [Ligand Id: 7000] activity data from GtoPdb and ChEMBL

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: CHEMBL140
  • acetylcholinesterase (Cartwright blood group)/Acetylcholinesterase in Human [ChEMBL: CHEMBL220] [GtoPdb: 2465] [UniProtKB: P22303]
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!
  • 5-LOX/Arachidonate 5-lipoxygenase in Human [ChEMBL: CHEMBL215] [GtoPdb: 1385] [UniProtKB: P09917]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • butyrylcholinesterase/Butyrylcholinesterase in Human [ChEMBL: CHEMBL1914] [GtoPdb: 2471] [UniProtKB: P06276]
There should be some charts here, you may need to enable JavaScript!
  • CDGSH iron-sulfur domain-containing protein 1 in Human [ChEMBL: CHEMBL1795168] [UniProtKB: Q9NZ45]
There should be some charts here, you may need to enable JavaScript!
  • coagulation factor III, tissue factor/Coagulation factor III in Human [ChEMBL: CHEMBL4081] [GtoPdb: 3192] [UniProtKB: P13726]
There should be some charts here, you may need to enable JavaScript!
  • CREB binding protein/CREB-binding protein in Human [ChEMBL: CHEMBL5747] [GtoPdb: 2734] [UniProtKB: Q92793]
There should be some charts here, you may need to enable JavaScript!
  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
There should be some charts here, you may need to enable JavaScript!
  • hydroxysteroid 17-beta dehydrogenase 2/Estradiol 17-beta-dehydrogenase 2 in Human [ChEMBL: CHEMBL2789] [GtoPdb: 3094] [UniProtKB: P37059]
There should be some charts here, you may need to enable JavaScript!
  • glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
  • glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Rat [ChEMBL: CHEMBL3669] [GtoPdb: 2030] [UniProtKB: P18266]
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!
  • E1A binding protein p300/Histone acetyltransferase p300 in Human [ChEMBL: CHEMBL3784] [GtoPdb: 2735] [UniProtKB: Q09472]
There should be some charts here, you may need to enable JavaScript!
  • histone deacetylase 1/Histone deacetylase 1 in Human [ChEMBL: CHEMBL325] [GtoPdb: 2658] [UniProtKB: Q13547]
There should be some charts here, you may need to enable JavaScript!
  • histone deacetylase 2/Histone deacetylase 2 in Human [ChEMBL: CHEMBL1937] [GtoPdb: 2616] [UniProtKB: Q92769]
There should be some charts here, you may need to enable JavaScript!
  • histone deacetylase 8/Histone deacetylase 8 in Human [ChEMBL: CHEMBL3192] [GtoPdb: 2619] [UniProtKB: Q9BY41]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • lysine demethylase 1A/Lysine-specific histone demethylase 1 in Human [ChEMBL: CHEMBL6136] [GtoPdb: 2669] [UniProtKB: O60341]
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!
  • NLRP3/NACHT, LRR and PYD domains-containing protein 3 in Human [ChEMBL: CHEMBL1741208] [GtoPdb: 1770] [UniProtKB: Q96P20]
There should be some charts here, you may need to enable JavaScript!
  • nuclear factor, erythroid 2 like 2/Nuclear factor erythroid 2-related factor 2 in Human [ChEMBL: CHEMBL1075094] [GtoPdb: 3057] [UniProtKB: Q16236]
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!
  • proteasome 20S subunit beta 5/Proteasome Macropain subunit MB1 in Human [ChEMBL: CHEMBL4662] [GtoPdb: 2406] [UniProtKB: P28074]
There should be some charts here, you may need to enable JavaScript!
  • Rhodesain in Trypanosoma brucei rhodesiense [ChEMBL: CHEMBL4188] [UniProtKB: Q95PM0]
There should be some charts here, you may need to enable JavaScript!
  • Sarcoplasmic/endoplasmic reticulum calcium ATP-ase in Rabbit [ChEMBL: CHEMBL4693] [UniProtKB: P04191]
There should be some charts here, you may need to enable JavaScript!
  • SERCA2/Sarcoplasmic/endoplasmic reticulum calcium ATPase 2 in Human [ChEMBL: CHEMBL3901] [GtoPdb: 841] [UniProtKB: P16615]
There should be some charts here, you may need to enable JavaScript!
  • SERCA3/Sarcoplasmic/endoplasmic reticulum calcium ATPase 3 in Human [ChEMBL: CHEMBL2401] [GtoPdb: 842] [UniProtKB: Q93084]
There should be some charts here, you may need to enable JavaScript!
  • p21 (RAC1) activated kinase 1/Serine/threonine-protein kinase PAK 1 in Human [ChEMBL: CHEMBL4600] [GtoPdb: 2133] [UniProtKB: Q13153]
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!
  • SRC proto-oncogene, non-receptor tyrosine kinase/Tyrosine-protein kinase SRC in Mouse [ChEMBL: CHEMBL3074] [GtoPdb: 2206] [UniProtKB: P05480]
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
acetylcholinesterase (Cartwright blood group)/Acetylcholinesterase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL220] [GtoPdb: 2465] [UniProtKB: P22303]
ChEMBL Inhibition of human erythrocyte AChE using acetylthiocholine chloride as substrate pretreated for 15 mins followed by substrate addition measured for 2 mins by DTNB reagent based spectrophotometric method B 5.3 pIC50 >5000 nM IC50 Eur J Med Chem (2017) 130: 139-153 [PMID:28242549]
Alpha-synuclein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6152] [UniProtKB: P37840]
ChEMBL Binding affinity to alpha-synuclein LMV 50 kDa (unknown origin) expressed in Escherichia coli BL21(DE3) cells incubated for 30 mins by spectrofluorometric analysis B 5.19 pKd 6500 nM Kd Eur J Med Chem (2019) 167: 10-36 [PMID:30743095]
ChEMBL Binding affinity to alpha-synuclein LMV 100 kDa (unknown origin) expressed in Escherichia coli BL21(DE3) cells incubated for 30 mins by spectrofluorometric analysis B 5.3 pKd 5000 nM Kd Eur J Med Chem (2019) 167: 10-36 [PMID:30743095]
ChEMBL Binding affinity to alpha-synuclein oligomer (unknown origin) expressed in Escherichia coli BL21(DE3) cells incubated for 30 mins by spectrofluorometric analysis B 5.7 pKd 2000 nM Kd Eur J Med Chem (2019) 167: 10-36 [PMID:30743095]
ChEMBL Binding affinity to alpha-synuclein preformed fibrils (unknown origin) expressed in Escherichia coli BL21(DE3) cells incubated for 30 mins by spectrofluorometric analysis B 6.3 pKd 500 nM Kd Eur J Med Chem (2019) 167: 10-36 [PMID:30743095]
ChEMBL Inhibition of alpha-synuclein fibril formation (unknown origin) incubated for 24 hrs to 7 days by thioflavin S based fluorescence assay B 6.66 pIC50 220 nM IC50 Eur J Med Chem (2019) 167: 10-36 [PMID:30743095]
Aminopeptidase N in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1907] [GtoPdb: 1560] [UniProtKB: P15144]
ChEMBL Inhibition of APN (unknown origin) B 4.81 pIC50 15500 nM IC50 J Med Chem (2018) 61: 6468-6490 [PMID:29630364]
5-LOX/Arachidonate 5-lipoxygenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL215] [GtoPdb: 1385] [UniProtKB: P09917]
ChEMBL Inhibition of human PMNL 5-LOX using arachidonic acid as substrate after 5 mins by HPLC method B 4.52 pIC50 30000 nM IC50 Bioorg Med Chem (2019) 27: 3745-3759 [PMID:31331653]
Beta amyloid A4 protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2487] [UniProtKB: P05067]
ChEMBL Inhibition of HFIP-pretreated amyloid beta (1 to 42 residues) (unknown origin) self aggregation after 24 hrs by ThT-based fluorometric method B 4.65 pIC50 22510 nM IC50 Eur J Med Chem (2017) 136: 36-51 [PMID:28478343]
ChEMBL Inhibition of HFIP-pretreated amyloid beta (1 to 42) (unknown origin) self-induced aggregation after 48 hrs by thioflavin-T fluorescence assay B 4.66 pIC50 21810 nM IC50 Eur J Med Chem (2017) 125: 736-750 [PMID:27721157]
ChEMBL Inhibition of self-induced amyloid beta (1 to 42) (unknown origin) aggregation incubated for 48 hrs measured after 5 mins by thioflavin-T fluorescence assay B 4.66 pIC50 21810 nM IC50 Bioorg. Med. Chem. (2016) 24: 3829-3841 [PMID:27353888]
ChEMBL Inhibition of HFIP-pretreated amyloid beta (1 to 42) (unknown origin) self-induced aggregation after 24 hrs by thioflavin-T fluorescence assay B 4.73 pIC50 18730 nM IC50 Bioorg Med Chem (2018) 26: 5759-5765 [PMID:30360953]
ChEMBL Inhibition of HFIP-pretreated amyloid beta (1 to 42) (unknown origin) self-induced aggregation incubated for 24 hrs under dark condition by thioflavin-T based fluorometric assay B 4.73 pIC50 18730 nM IC50 Eur J Med Chem (2017) 127: 174-186 [PMID:28061347]
ChEMBL Inhibition of self-mediated amyloid beta (1 to 42) (unknown origin) aggregation after 48 hrs by thioflavin T fluorescence assay B 4.74 pIC50 18250 nM IC50 Eur J Med Chem (2016) 122: 17-26 [PMID:27343850]
ChEMBL Inhibition of amyloid beta (1 to 42) (unknown origin) self aggregation incubated for 48 hrs by thioflavin-T fluorescence method B 4.79 pIC50 16250 nM IC50 Bioorg Med Chem Lett (2020) 30: 127659-127659 [PMID:33137375]
ChEMBL Inhibition of amyloid beta (1 to 42) (unknown origin) self-aggregation after 24 hrs by thioflavin-T fluorescence assay B 4.82 pIC50 14990 nM IC50 Eur J Med Chem (2018) 151: 351-362 [PMID:29635167]
ChEMBL Inhibition of self-induced aggregation of amyloid beta (1 to 42) (unknown origin) after 48 hrs by thioflavin T-based fluorescence method B 4.86 pIC50 13700 nM IC50 MedChemComm (2018) 9: 1862-1870 [PMID:30568754]
ChEMBL Inhibition of self-mediated amyloid beta (1 to 42) (unknown origin) aggregation after 10 hrs by thioflavin T based fluorometric assay B 4.95 pIC50 11300 nM IC50 Bioorg. Med. Chem. Lett. (2016) 26: 747-750 [PMID:26783181]
ChEMBL Inhibition of human amyloid beta (1 to 42) aggregation after 46 to 48 hrs by Thioflavin T fluorescence assay B 5 pIC50 10000 nM IC50 J Nat Prod (2017) 80: 278-289 [PMID:28128562]
ChEMBL Inhibition of HFIP-induced human recombinant amyloid beta (1 to 42 residues) aggregation expressed in Escherichia coli measured over 24 hrs by ThT-based fluorescence spectroscopic method B 5 pIC50 9900 nM IC50 Eur J Med Chem (2017) 126: 823-843 [PMID:27951490]
ChEMBL Inhibition of HFIP-pretreated amyloid beta (1 to 42 residues) (unknown origin) aggregation after 24 hrs by ThT fluorescence assay B 5.05 pIC50 9000 nM IC50 Bioorg Med Chem Lett (2017) 27: 1405-1411 [PMID:28216401]
ChEMBL Inhibition of Abeta42 (unknown origin) aggregation measured after 24 hrs by ThT fluorescence assay B 5.05 pIC50 9000 nM IC50 Bioorg. Med. Chem. Lett. (2016) 26: 3330-3335 [PMID:27256911]
ChEMBL Inhibition of amyloid beta (1 to 42) (unknown origin) self-induced aggregation incubated for 24 hrs by Thioflavin T based fluorometric assay B 5.08 pIC50 8270 nM IC50 Bioorg Med Chem (2021) 44: 116306-116306 [PMID:34274550]
ChEMBL Inhibition of amyloid beta (1 to 42) (unknown origin) self aggregation B 5.19 pIC50 6385 nM IC50 Eur J Med Chem (2019) 180: 656-672 [PMID:31352246]
ChEMBL Inhibition of amyloid beta (1 to 42 residues) (unknown origin) aggregation after 24 hrs by thioflavin T fluorescence assay B 5.27 pIC50 5400 nM IC50 Bioorg Med Chem Lett (2016) 26: 5024-5028 [PMID:27624076]
ChEMBL Inhibition of human biotinylated amyloid beta (1 to 42) oligomerization assessed as decrease in oligomer abundance measured after 1 hr by ELISA B 5.41 pIC50 3850 nM IC50 Bioorg Med Chem (2021) 43: 116247-116247 [PMID:34157569]
ChEMBL Inhibition of amyloid beta (1 to 42) fibrillization (unknown origin) incubated with agitation for 1 min every hr measured over 80 hrs by thioflavin-T assay B 5.47 pIC50 3400 nM IC50 Eur J Med Chem (2018) 158: 393-404 [PMID:30227353]
ChEMBL Inhibition of HFIP-induced human recombinant amyloid beta (1 to 40 residues) aggregation expressed in Escherichia coli measured over 24 hrs by ThT-based fluorescence spectroscopic method B 5.48 pIC50 3300 nM IC50 Eur J Med Chem (2017) 126: 823-843 [PMID:27951490]
ChEMBL Inhibition of self-induced amyloid beta 42 (unknown origin) aggregation measured for 24 hrs by thioflavin T-based fluorescence spectroscopic analysis B 5.51 pIC50 3100 nM IC50 ACS Med. Chem. Lett. (2016) 7: 502-507 [PMID:27190601]
ChEMBL Inhibition of self-induced amyloid beta 40 (unknown origin) aggregation measured for 24 hrs by thioflavin T-based fluorescence spectroscopic analysis B 5.82 pIC50 1500 nM IC50 ACS Med. Chem. Lett. (2016) 7: 502-507 [PMID:27190601]
ChEMBL Inhibition of amyloid beta (1 to 40 residues) (unknown origin) fibril formation by thioflavin-T fluorescence based assay B 6 pIC50 1000 nM IC50 J Med Chem (2017) 60: 1620-1637 [PMID:28074653]
ChEMBL Inhibition of human amyloid beta (1 to 40) aggregation after 1 hr by thioflavin-T fluorescence assay B 6.1 pIC50 800 nM IC50 J Nat Prod (2017) 80: 278-289 [PMID:28128562]
ChEMBL Inhibition of amyloid beta (1 to 42) aggregation (unknown origin) by ThT fluorescence assay B 6.2 pIC50 630 nM IC50 Bioorg Med Chem (2017) 25: 1195-1201 [PMID:28043778]
butyrylcholinesterase/Butyrylcholinesterase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1914] [GtoPdb: 2471] [UniProtKB: P06276]
ChEMBL Inhibition of human serum BuChE using butylthiocholine chloride as substrate pretreated for 15 mins followed by substrate addition measured for 2 mins by DTNB reagent based spectrophotometric method B 5.3 pIC50 >5000 nM IC50 Eur J Med Chem (2017) 130: 139-153 [PMID:28242549]
CDGSH iron-sulfur domain-containing protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795168] [UniProtKB: Q9NZ45]
ChEMBL Displacement of [3H]rosiglitazone from recombinant human C-terminal His-tagged MitoNEET cytosolic domain (32 to 108 residues) expressed in Escherichia coli BL21 by Cheng-Prusoff analysis B 7 pKi 101 nM Ki Bioorg Med Chem Lett (2016) 26: 5350-5353 [PMID:27687671]
ChEMBL Displacement of [3H]rosiglitazone from recombinant human C-terminal His-tagged MitoNEET cytosolic domain (32 to 108 residues) expressed in Escherichia coli BL21 by scintillation proximity assay B 5.63 pIC50 2360 nM IC50 Bioorg Med Chem Lett (2016) 26: 5350-5353 [PMID:27687671]
coagulation factor III, tissue factor/Coagulation factor III in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4081] [GtoPdb: 3192] [UniProtKB: P13726]
ChEMBL Inhibition of LPS-induced tissue factor procoagulant activity in human THP1 cells preincubated for 1 hr followed by LPS addition measured after 5 hrs using factor 10a chromogenic substrate in presence of prothrombin complex B 7.88 pIC50 13.16 nM IC50 Bioorg Med Chem Lett (2017) 27: 1026-1030 [PMID:28109788]
CREB binding protein/CREB-binding protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5747] [GtoPdb: 2734] [UniProtKB: Q92793]
ChEMBL Inhibition of recombinant CBP (unknown origin) expressed in baculovirus expression system using histone substrate after 10 mins by liquid scintillation counting method in presence of [3H]acetyl-CoA B 4.6 pIC50 25000 nM IC50 J. Med. Chem. (2016) 59: 1249-1270 [PMID:26701186]
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
ChEMBL Time-Resolved Fluorescence Assay: The kinase activity of EGFR was detected according to time-resolved fluorescence detection technology to evaluate automatic phosphorylation levels. The test compound was dissolved in 100% DMSO, diluted with 25 mM HEPES (pH=7.4) to the desired concentration, added into each well with 10 μL of the test compounds and 10 μL solution containing 5 ng EGFR, then cultured for 10 min at room temperature using the recombinase diluted by 100 mM HEPES with a dilution ratio of 1:80, subsequently added with 10 μL solution containing 20 mM HEPES, 2 mM MnCl2, 100 μM Na3VO4, 1 mM DTT buffer, and 20 μL of 0.1 mM ATP and 50 mM MgCl2 and cultured for 1 h. The positive group in each plate was added with ATP-MgCl2 enzyme, the negative control group without adding with ATP-MgCl2 enzyme, the liquid was sucked out completely after cultured for 1 h, and each well was washed with buffer for three times. The wells were added with 75 μL anti-phosphorylated tyrosine antibody containing 400 ng europium labeling and cultured 1 h, washed, then added with enhancing solution. At the excitation wavelength 340 nm and the emission wavelength 615 nm, the fluorescence intensities were detected by using Victor type 2 time-resolved luminoscope, wherein the inhibitory rate of the compound on automatic phosphorylation: the inhibitory rate of autophosphorylation=100%−[(negative control)/(positive control−negative control)]. B 5.06 pIC50 8650 nM IC50 US-9409845-B2. Alpha-(3,5-dimethoxybenzylidene)-alpha′-hydrocarbyl methylene cyclic ketone and preparation method thereof (2016)
hydroxysteroid 17-beta dehydrogenase 2/Estradiol 17-beta-dehydrogenase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2789] [GtoPdb: 3094] [UniProtKB: P37059]
ChEMBL Inhibition of human 17beta-HSD2 expressed in HEK293 cell lysates incubated for 10 mins using [2,4,6,7-3H]-estradiol and NAD+ by scintillation counting method B 5.76 pIC50 1730 nM IC50 J Nat Prod (2017) 80: 965-974 [PMID:28319389]
glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
ChEMBL Inhibition of human recombinant GSK3-beta using prephosphorylated polypeptide as substrate incubated for 30 mins by Glo-type luminescence assay B 4.75 pIC50 17950 nM IC50 J. Med. Chem. (2016) 59: 531-544 [PMID:26696252]
glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3669] [GtoPdb: 2030] [UniProtKB: P18266]
ChEMBL Inhibition of recombinant rat N-terminal GST-tagged GSK3beta expressed in Escherichia coli assessed as reduction in tau phosphorylation preincubated for 30 mins followed by tau protein addition measured after 1 hr by ELISA B 7.18 pIC50 66 nM IC50 J Med Chem (2017) 60: 1620-1637 [PMID:28074653]
Glyoxalase I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2424] [UniProtKB: Q04760]
ChEMBL Inhibition of human erythrocyte Glyoxalase-1 using GSH and MGO as substrate by Dixon plot analysis B 8.3 pKi 5 nM Ki Bioorg Med Chem (2020) 28: 115243-115243 [PMID:31879183]
GroEL/GroES in Escherichia coli (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4106139] [UniProtKB: Q548M1, Q7BGE6]
ChEMBL Inhibition of Escherichia coli GroEL expressed in Escherichia coliDH5alpha/Escherichia coli GroES expressed in Escherichia coli BL21 (DE3) assessed as reduction in GroEL/GroES-mediated denatured soluble pig heart MDH refolding by measuring MDH enzyme activity using sodium mesoxalate as substrate after 20 to 40 mins by malachite green dye based spectrometric analysis B 5.51 pIC50 3100 nM IC50 Bioorg Med Chem Lett (2019) 29: 1106-1112 [PMID:30852084]
ChEMBL Inhibition of Escherichia coli GroEL expressed in Escherichia coli DH5alpha/Escherichia coli GroES expressed in Escherichia coli BL21 (DE3) assessed as reduction in GroEL/GroES-mediated denatured rhodanese refolding by measuring rhodanese enzyme activity after 45 mins by Fe(SCN)3 dye based spectrometric analysis B 5.54 pIC50 2900 nM IC50 Bioorg Med Chem Lett (2019) 29: 1106-1112 [PMID:30852084]
E1A binding protein p300/Histone acetyltransferase p300 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3784] [GtoPdb: 2735] [UniProtKB: Q09472]
GtoPdb - - 4.6 pIC50 25000 nM IC50 J Biol Chem (2004) 279: 51163-71 [PMID:15383533]
ChEMBL Inhibition of recombinant p300 (unknown origin) expressed in baculovirus expression system using histone substrate after 10 mins by liquid scintillation counting method in presence of [3H]acetyl-CoA B 4.6 pIC50 25000 nM IC50 J. Med. Chem. (2016) 59: 1249-1270 [PMID:26701186]
ChEMBL Inhibition of recombinant human full-length His6-tagged p300 expressed in baculovirus infected Sf21 insect cells using [3H]acetylCoA as substrate preincubated for 10 mins followed by substrate addition and measured after 10 mins by liquid scintillation counting method B 4.6 pIC50 25000 nM IC50 J Med Chem (2020) 63: 1337-1360 [PMID:31910017]
ChEMBL Inhibition of recombinant human p300 catalytic domain (1284 to 1673 residues) using histone H3 peptide substrate after 1 hr by liquid scintillation counting method in presence of [3H]acetyl-CoA B 5.19 pIC50 6500 nM IC50 J. Med. Chem. (2016) 59: 1249-1270 [PMID:26701186]
histone deacetylase 1/Histone deacetylase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL325] [GtoPdb: 2658] [UniProtKB: Q13547]
ChEMBL Inhibition of HDAC1 (unknown origin) B 4.29 pKi 50790 nM Ki Bioorg Med Chem Lett (2020) 30: 127171-127171 [PMID:32273215]
histone deacetylase 2/Histone deacetylase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1937] [GtoPdb: 2616] [UniProtKB: Q92769]
ChEMBL Inhibition of HDAC2 (unknown origin) B 4.01 pKi 97670 nM Ki Bioorg Med Chem Lett (2020) 30: 127171-127171 [PMID:32273215]
histone deacetylase 8/Histone deacetylase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3192] [GtoPdb: 2619] [UniProtKB: Q9BY41]
ChEMBL Inhibition of HDAC8 (unknown origin) B 4.19 pKi 64980 nM Ki Bioorg Med Chem Lett (2020) 30: 127171-127171 [PMID:32273215]
HSP60/HSP10 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4106131] [UniProtKB: P10809, P61604]
ChEMBL Inhibition of human N-terminal octa-His-tagged HSP60 expressed in Escherichia coli Rosetta(DE3) pLysS/human HSP10 expressed in Escherichia coli Rosetta(DE3) assessed as reduction in HSP60/HSP10-mediated denatured MDH refolding by measuring MDH enzyme activity using sodium mesoxalate as substrate after 40 to 60 mins by malachite green dye based spectrometric analysis B 5.08 pIC50 8300 nM IC50 Bioorg Med Chem Lett (2019) 29: 1106-1112 [PMID:30852084]
lysine demethylase 1A/Lysine-specific histone demethylase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6136] [GtoPdb: 2669] [UniProtKB: O60341]
ChEMBL Inhibition of human recombinant LSD1 using fluorogenic ADHP as substrate preincubated for 30 mins followed by substrate addition measured after 10 mins by fluorescence assay B 5.02 pIC50 9600 nM IC50 Bioorg Med Chem Lett (2019) 29: 126683-126683 [PMID:31627991]
Microtubule-associated protein tau in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293224] [UniProtKB: P10636]
ChEMBL Inhibition of tau (unknown origin) fibril formation by fluorescence assay B 4.89 pIC50 13000 nM