MMV019313 [Ligand Id: 11456] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL532155 (MMV019313, TCMDC-123889)
  • Calcium-dependent protein kinase 1 in Plasmodium falciparum 3D7 [ChEMBL: CHEMBL1908387] [UniProtKB: P62344]
  • This target only has 0 pki data point
  • 0
1 CHEMBL532155_lig_chart_1 Calcium-dependent protein kinase 1 Plasmodium falciparum 3D7
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  • Calcium-dependent protein kinase 4 in Plasmodium falciparum 3D7 [ChEMBL: CHEMBL2169725] [UniProtKB: Q8IBS5]
  • This target only has 0 pki data point
  • 0
2 CHEMBL532155_lig_chart_2 Calcium-dependent protein kinase 4 Plasmodium falciparum 3D7
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  • Cdk-related protein kinase 6 in Plasmodium falciparum [ChEMBL: CHEMBL3301558] [UniProtKB: O77239]
  • This target only has 0 pki data point
  • 0
3 CHEMBL532155_lig_chart_3 Cdk-related protein kinase 6 Plasmodium falciparum
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  • Glucose transporter in Leishmania mexicana [ChEMBL: CHEMBL3431938] [UniProtKB: O61059]
  • Glucose transporter 1/Glucose transporter in Human [ChEMBL: CHEMBL2535] [GtoPdb: 875] [UniProtKB: P11166]
  • This target only has 0 pki data point
  • 0
4 CHEMBL532155_lig_chart_4 Glucose transporter Leishmania mexicanaHuman
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  • Hexose transporter 1 in Plasmodium falciparum [ChEMBL: CHEMBL4697] [UniProtKB: O97467]
  • This target only has 0 pki data point
  • 0
5 CHEMBL532155_lig_chart_5 Hexose transporter 1 Plasmodium falciparum
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  • Plasmodium falciparum lysine--tRNA ligase/Lysine--tRNA ligase in Plasmodium falciparum 3D7 [ChEMBL: CHEMBL3301561] [GtoPdb: 3059] [UniProtKB: Q8IDJ8]
  • This target only has 0 pki data point
  • 0
6 CHEMBL532155_lig_chart_6 Lysine--tRNA ligase Plasmodium falciparum 3D7
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  • Mitogen-activated protein kinase in Plasmodium falciparum [ChEMBL: CHEMBL3301559] [UniProtKB: Q25917]
  • This target only has 0 pki data point
  • 0
7 CHEMBL532155_lig_chart_7 Mitogen-activated protein kinase Plasmodium falciparum
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  • Plasmodium falciparum [ChEMBL: CHEMBL364]
  • This target only has 0 pki data point
  • 0
8 CHEMBL532155_lig_chart_8 Plasmodium falciparum Plasmodium falciparum
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  • Plasmodium falciparum proline--tRNA ligase/Proline--tRNA ligase in Plasmodium falciparum 3D7 [ChEMBL: CHEMBL3301560] [GtoPdb: 3056] [UniProtKB: Q8I5R7]
  • This target only has 0 pki data point
  • 0
9 CHEMBL532155_lig_chart_9 Proline--tRNA ligase Plasmodium falciparum 3D7
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  • Putative uncharacterized protein pk7 in Plasmodium falciparum [ChEMBL: CHEMBL6169] [UniProtKB: O96214]
  • This target only has 0 pki data point
  • 0
10 CHEMBL532155_lig_chart_10 Putative uncharacterized protein pk7 Plasmodium falciparum
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  • Plasmodium falciparum bifunctional farnesyl/geranylgeranyl diphosphate synthase in Plasmodium falciparum W2 [GtoPdb: 3173]
  • Plasmodium falciparum bifunctional farnesyl/geranylgeranyl diphosphate synthase in Plasmodium falciparum Dd2 [GtoPdb: 3173]
  • This target only has 0 pki data point
  • 0
11 CHEMBL532155_lig_chart_11 Plasmodium falciparum bifunctional farnesyl/geranylgeranyl diphosphate synthase Plasmodium falciparum W2Plasmodium falciparum Dd2
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Calcium-dependent protein kinase 1 in Plasmodium falciparum 3D7 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1908387] [UniProtKB: P62344]
ChEMBL MMV: CDPK1 Protein kinase inhibition assay using recombinant PfCDPK1, syntide 2 peptide substrate, ATP and KinaseGlo to measure % inhibition at 1 uM MMV box compound. F 6 pIC50 >1000 nM IC50 MMV Box screening against Plasmodium falciparum protein kinases and aminoacyl tRNA synthetases.
Calcium-dependent protein kinase 4 in Plasmodium falciparum 3D7 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2169725] [UniProtKB: Q8IBS5]
ChEMBL MMV: CDPK4 Protein kinase inhibition assay using recombinant PfCDPK4, syntide2 peptide substrate, ATP and KinaseGlo to measure % inhibition at 1 uM MMV box compound. F 6 pIC50 >1000 nM IC50 MMV Box screening against Plasmodium falciparum protein kinases and aminoacyl tRNA synthetases.
Cdk-related protein kinase 6 in Plasmodium falciparum (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3301558] [UniProtKB: O77239]
ChEMBL MMV: PK6 Protein kinase inhibition assay using recombinant PfPK6, Myelin Basic Protein (MBP) substrate, ATP and KinaseGlo to measure % inhibition at 1 uM MMV box compound. Final concentrations were 1.5 uM ATP, 5 mM MnCl2, and 15 ug/ml PK6 in a buffer of 100 mM Tris-HCl (pH 7.5). 50 ug/mL MBP was provided as the substrate; 10 uM staurosporine was used as a control inhibitor. Incubation time was 3 hours and 40 minutes.The catalytic activity of each kinase was considered proportional to ATP consumed, as determined from measurements of residual [ATP] with the luciferase-based reagent Kinase-Glo (Promega) following incubation. Luminescence (proportional to residual [ATP]) was measured on the plate readers FLx800 (BioTek Instruments, Winooski, VT, USA) and MicroBeta2. F 6 pIC50 >1000 nM IC50 MMV Box screening against Plasmodium falciparum protein kinases and aminoacyl tRNA synthetases.
Glucose transporter in Leishmania mexicana (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3431938] [UniProtKB: O61059]
ChEMBL ST_JUDE_LEISH: Cytotoxicity against transgenic Leishmania Mexicana promastigotes LmGT2 that are glucose transport deficient and complemented with the L. Mexicana glucose transporter 2. Activity is measured by by DNA content using SYBR green in vitro F 4.92 pIC50 >12000 nM IC50 St. Jude Leishmania screening dataset.
Glucose transporter 1/Glucose transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2535] [GtoPdb: 875] [UniProtKB: P11166]
ChEMBL ST_JUDE_LEISH: Cytotoxicity against transgenic Leishmania Mexicana promastigotes LmGLUT1 that are glucose transport deficient and complemented with the human glucose transporter GLUT1. Activity is measured by DNA content using SYBR green in vitro F 4.92 pIC50 >12000 nM IC50 St. Jude Leishmania screening dataset.
Hexose transporter 1 in Plasmodium falciparum (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4697] [UniProtKB: O97467]
ChEMBL ST_JUDE_LEISH: Cytotoxicity against transgenic Leishmania Mexicana promastigotes LmPfHT that are glucose transport deficient and complemented with the Plasmodium falciparum hexose transporter. Activity is measured by by DNA content using SYBR green in vitro F 4.92 pIC50 >12000 nM IC50 St. Jude Leishmania screening dataset.
Plasmodium falciparum lysine--tRNA ligase/Lysine--tRNA ligase in Plasmodium falciparum 3D7 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3301561] [GtoPdb: 3059] [UniProtKB: Q8IDJ8]
ChEMBL MMV: KRS recombinant Plasmodium falciparum Lysyl-tRNA-synthetase, assay with yeast tRNA, ATP, and lysine and 3 uM MMV malaria box compound, assay read out with kinase glo as % inhibition. F 5.6 pIC50 >2500 nM IC50 MMV Box screening against Plasmodium falciparum protein kinases and aminoacyl tRNA synthetases.
Mitogen-activated protein kinase in Plasmodium falciparum (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3301559] [UniProtKB: Q25917]
ChEMBL MMV: MAP2K Protein kinase inhibition assay using recombinant PfMAP2K, protein substrate, ATP and KinaseGlo to measure % inhibition at 1 uM MMV box compound. Final concentrations were 1 uM ATP, 0.5 mM DTT, 1 mM MgCl2, 0.5 mg/mL BSA, and 10 ug/ml MAP2 in a buffer of 50 mM HEPES (pH 7.0). 0.5 mg/mL histone III-S served as the substrate (13); 100 uM AMP-PNP, an ATP analog, was used as a control inhibitor. Incubation time was 4 hours. F 6 pIC50 >1000 nM IC50 MMV Box screening against Plasmodium falciparum protein kinases and aminoacyl tRNA synthetases.
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL MMV: IC50 determined against P. falciparum Dd2-luc strain using a Malaria Sybr Green I Fluorescence assay. Starting conditions were 1% trophozoite synchronised parasites at 2% haematocrit. Fluorescence detection completed after 48hr incubation at 37 degrees C under 1% O2, 3% CO2 and balance N2. F 6.44 pIC50 366.4 nM IC50 MMV box screening in the Dd2 P. falciparum strain
ChEMBL MMV: Inhibition of Plasmodium falciparum 3D7 (EC50). F 6.17 pEC50 669 nM EC50 Malaria Box
ChEMBL MMV: Inhibition of Plasmodium falciparum K1 (EC50). F 6.24 pEC50 576 nM EC50 Malaria Box
Plasmodium falciparum proline--tRNA ligase/Proline--tRNA ligase in Plasmodium falciparum 3D7 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3301560] [GtoPdb: 3056] [UniProtKB: Q8I5R7]
ChEMBL MMV: ProRS recombinant Plasmodium falciparum Prolyl-tRNA-synthetase, assay with yeast tRNA, ATP, and proline and 3 uM MMV malaria box compound, assay read out with kinase glo as % inhibition. F 5.6 pIC50 >2500 nM IC50 MMV Box screening against Plasmodium falciparum protein kinases and aminoacyl tRNA synthetases.
Putative uncharacterized protein pk7 in Plasmodium falciparum (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6169] [UniProtKB: O96214]
ChEMBL MMV: PK7 Protein kinase inhibition assay using recombinant PfPK7, ATP and KinaseGlo to measure % inhibition at 1 uM MMV box compound. Final concentrations were 1 uM ATP, 2 mM DTT, 20 mM MgCl2, 2 mM MnCl2, 0.01% BSA, and 6 ug/ml PK7, in a buffer of 20 mM Tris-HCl (pH 7.5). The enzyme itself was the only substrate present (since autophosphorylation occurs); 100 uM 1NA-PP1 was used as a control inhibitor. Incubation time was 3 hours. F 6 pIC50 >1000 nM IC50 MMV Box screening against Plasmodium falciparum protein kinases and aminoacyl tRNA synthetases.
Plasmodium falciparum bifunctional farnesyl/geranylgeranyl diphosphate synthase in Plasmodium falciparum W2 [GtoPdb: 3173]
GtoPdb - - 6.57 pEC50 270 nM EC50 Cell Chem Biol (2018) 25: 185-193.e5 [PMID:29276048]
Plasmodium falciparum bifunctional farnesyl/geranylgeranyl diphosphate synthase in Plasmodium falciparum Dd2 [GtoPdb: 3173]
GtoPdb - - 6.74 pEC50 180 nM EC50 Cell Chem Biol (2018) 25: 185-193.e5 [PMID:29276048]

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]