BMS-509744 [Ligand Id: 9994] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL209148 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| calcium/calmodulin-dependent protein kinase II alpha subunit/Calcium/calmodulin-dependent protein kinase type II subunit alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4147] [GtoPdb: 1555] [UniProtKB: Q9UQM7] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (radiometric inhibition assay)) EUB0000651a CAMK2A | B | 4.47 | pIC50 | 33500 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| protein kinase, cAMP-dependent, catalytic, alpha subunit/cAMP-dependent protein kinase catalytic subunit alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4101] [GtoPdb: 1476] [UniProtKB: P17612] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (radiometric inhibition assay)) EUB0000651a PRKACA | B | 4.3 | pIC50 | >50000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941] | ||||||||
| ChEMBL | Inhibition of Cdk2 | B | 4.54 | pIC50 | 29000 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 3706-3712 [PMID:16682193] |
| ChEMBL | Selectivity interaction (Kinase panel (radiometric inhibition assay)) EUB0000651a CDK2 | B | 4.54 | pIC50 | 29000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Inhibition of Cdk2 (unknown origin) using GST-SLP-76 as peptide substrate incubated for 10 mins in presence of [gamma-33P]ATP by scintillation counter assay | B | 4.54 | pIC50 | 29000 | nM | IC50 | Biochemistry (2004) 43: 11056-11062 [PMID:15323564] |
| BMX non-receptor tyrosine kinase/Cytoplasmic tyrosine-protein kinase BMX in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3834] [GtoPdb: 1942] [UniProtKB: P51813] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (radiometric inhibition assay)) EUB0000651a BMX | B | 4.3 | pIC50 | >50000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Inhibition of Bmx (unknown origin) using GST-SLP-76 as peptide substrate incubated for 10 mins in presence of [gamma-33P]ATP by scintillation counter assay | B | 4.3 | pIC50 | >50000 | nM | IC50 | Biochemistry (2004) 43: 11056-11062 [PMID:15323564] |
| epidermal growth factor receptor/Epidermal growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533] | ||||||||
| ChEMBL | Inhibition of EGFR | B | 4.3 | pIC50 | >50000 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 3706-3712 [PMID:16682193] |
| ChEMBL | Selectivity interaction (Kinase panel (radiometric inhibition assay)) EUB0000651a EGFR | B | 4.3 | pIC50 | >50000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Inhibition of EGFR (unknown origin) using GST-SLP-76 as peptide substrate incubated for 10 mins in presence of [gamma-33P]ATP by scintillation counter assay | B | 4.3 | pIC50 | >50000 | nM | IC50 | Biochemistry (2004) 43: 11056-11062 [PMID:15323564] |
| 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 GSK3-beta | B | 4.44 | pIC50 | 36000 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 3706-3712 [PMID:16682193] |
| ChEMBL | Selectivity interaction (Kinase panel (radiometric inhibition assay)) EUB0000651a GSK3B | B | 4.44 | pIC50 | 36000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Inhibition of GSK-3beta (unknown origin) using GST-SLP-76 as peptide substrate incubated for 10 mins in presence of [gamma-33P]ATP by scintillation counter assay | B | 4.44 | pIC50 | 36000 | nM | IC50 | Biochemistry (2004) 43: 11056-11062 [PMID:15323564] |
| inhibitor of nuclear factor kappa B kinase subunit beta/Inhibitor of nuclear factor kappa-B kinase subunit beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1991] [GtoPdb: 2039] [UniProtKB: O14920] | ||||||||
| ChEMBL | Inhibition of IKK-beta | B | 4.3 | pIC50 | >50000 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 3706-3712 [PMID:16682193] |
| ChEMBL | Selectivity interaction (Kinase panel (radiometric inhibition assay)) EUB0000651a IKBKB | B | 4.3 | pIC50 | >50000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Inhibition of IKKbeta (unknown origin) using GST-SLP-76 as peptide substrate incubated for 10 mins in presence of [gamma-33P]ATP by scintillation counter assay | B | 4.3 | pIC50 | >50000 | nM | IC50 | Biochemistry (2004) 43: 11056-11062 [PMID:15323564] |
| Insulin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1981] [GtoPdb: 1800] [UniProtKB: P06213] | ||||||||
| ChEMBL | Inhibition of Insulin receptor | B | 5.96 | pIC50 | 1100 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 3706-3712 [PMID:16682193] |
| ChEMBL | Selectivity interaction (Kinase panel (radiometric inhibition assay)) EUB0000651a INSR | B | 5.96 | pIC50 | 1100 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Inhibition of IR (unknown origin) using GST-SLP-76 as peptide substrate incubated for 10 mins in presence of [gamma-33P]ATP by scintillation counter assay | B | 5.96 | pIC50 | 1100 | nM | IC50 | Biochemistry (2004) 43: 11056-11062 [PMID:15323564] |
| Interleukin-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5880] [UniProtKB: P60568] | ||||||||
| ChEMBL | Inhibition of IL-2 in human Jurkat T cells pretreated with compound for 16 hrs followed by anti-CD3 stimulation by ELISA analysis | B | 6.62 | pEC50 | 237.6 | nM | EC50 | J Med Chem (2023) 66: 4979-4998 [PMID:36959108] |
| leukocyte receptor tyrosine kinase/Leukocyte tyrosine kinase receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5627] [GtoPdb: 1838] [UniProtKB: P29376] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (radiometric inhibition assay)) EUB0000651a LTK | B | 5.62 | pIC50 | 2400 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| mitogen-activated protein kinase 3/Mitogen-activated protein kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3385] [GtoPdb: 1494] [UniProtKB: P27361] | ||||||||
| ChEMBL | Inhibition of ERK1 | B | 4.3 | pIC50 | >50000 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 3706-3712 [PMID:16682193] |
| ChEMBL | Selectivity interaction (Kinase panel (radiometric inhibition assay)) EUB0000651a MAPK3 | B | 4.3 | pIC50 | >50000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Inhibition of ERK-1 (unknown origin) using GST-SLP-76 as peptide substrate incubated for 10 mins in presence of [gamma-33P]ATP by scintillation counter assay | B | 4.3 | pIC50 | >50000 | nM | IC50 | Biochemistry (2004) 43: 11056-11062 [PMID:15323564] |
| protein kinase C alpha/Protein kinase C alpha type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL299] [GtoPdb: 1482] [UniProtKB: P17252] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (radiometric inhibition assay)) EUB0000651a PRKCA | B | 4.62 | pIC50 | 24000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| AKT serine/threonine kinase 1/RAC-alpha serine/threonine-protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749] | ||||||||
| ChEMBL | Inhibition of Akt1 | B | 4.3 | pIC50 | >50000 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 3706-3712 [PMID:16682193] |
| ChEMBL | Selectivity interaction (Kinase panel (radiometric inhibition assay)) EUB0000651a AKT1 | B | 4.3 | pIC50 | >50000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Inhibition of Akt1 (unknown origin) using GST-SLP-76 as peptide substrate incubated for 10 mins in presence of [gamma-33P]ATP by scintillation counter assay | B | 4.3 | pIC50 | >50000 | nM | IC50 | Biochemistry (2004) 43: 11056-11062 [PMID:15323564] |
| Bruton tyrosine kinase/Tyrosine-protein kinase BTK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5251] [GtoPdb: 1948] [UniProtKB: Q06187] | ||||||||
| ChEMBL | Inhibition of Btk | B | 5.39 | pIC50 | 4100 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 3706-3712 [PMID:16682193] |
| ChEMBL | Selectivity interaction (Kinase panel (radiometric inhibition assay)) EUB0000651a BTK | B | 5.39 | pIC50 | 4100 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Inhibition of Btk (unknown origin) using GST-SLP-76 as peptide substrate incubated for 10 mins in presence of [gamma-33P]ATP by scintillation counter assay | B | 5.39 | pIC50 | 4100 | nM | IC50 | Biochemistry (2004) 43: 11056-11062 [PMID:15323564] |
| FYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Fyn in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1841] [GtoPdb: 2026] [UniProtKB: P06241] | ||||||||
| ChEMBL | Inhibition of Fyn | B | 5.96 | pIC50 | 1100 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 3706-3712 [PMID:16682193] |
| ChEMBL | Selectivity interaction (Kinase panel (radiometric inhibition assay)) EUB0000651a FYN | B | 5.96 | pIC50 | 1100 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Inhibition of Fyn (unknown origin) using GST-SLP-76 as peptide substrate incubated for 10 mins in presence of [gamma-33P]ATP by scintillation counter assay | B | 5.96 | pIC50 | 1100 | nM | IC50 | Biochemistry (2004) 43: 11056-11062 [PMID:15323564] |
| IL2 inducible T cell kinase/Tyrosine-protein kinase ITK/TSK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2959] [GtoPdb: 2046] [UniProtKB: Q08881] | ||||||||
| ChEMBL | Inhibition of ITK | B | 7.8 | pKi | 16 | nM | Ki | Chem Biol (2005) 12: 621-637 [PMID:15975507] |
| ChEMBL | Inhibition of Itk in LPS induced human PBMC cells assessed as inhibition of TNF alpha production | B | 4.6 | pIC50 | >25000 | nM | IC50 | Biochemistry (2004) 43: 11056-11062 [PMID:15323564] |
| ChEMBL | Inhibition of Itk in human Jurkat T cells assessed as inhibition of Ca2+ mobilization incubated for 30 mins in presence of anti-CD3 antibody G19-4 by fluo-3 AM based fluorometric imaging analysis | B | 5.88 | pIC50 | 1310 | nM | IC50 | Biochemistry (2004) 43: 11056-11062 [PMID:15323564] |
| ChEMBL | Affinity Phenotypic Cellular interaction: (T-cell proliferation induced by the mixed lymphocyte reaction) EUB0000651a ITK | F | 6.37 | pIC50 | 430 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity Phenotypic Cellular interaction: (nhibition of IL-2 secretion (in human PBMCs)) EUB0000651a ITK | F | 6.41 | pIC50 | 390 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Inhibition of Itk in human PBMC cells assessed as inhibition of IL-2 secretion incubated for 16 hrs in presence of anti-CD3 antibody G19-4 by ELISA analysis | B | 6.41 | pIC50 | 390 | nM | IC50 | Biochemistry (2004) 43: 11056-11062 [PMID:15323564] |
| ChEMBL | Affinity Phenotypic Cellular interaction: (Inhibition of IL-2 Secretion in Jurkat cells) EUB0000651a ITK | F | 6.6 | pIC50 | 250 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Inhibition of Itk in human Jurkat T cells assessed as inhibition of IL-2 secretion incubated for 16 hrs in presence of anti-CD3 antibody G19-4 by ELISA analysis | B | 6.6 | pIC50 | 250 | nM | IC50 | Biochemistry (2004) 43: 11056-11062 [PMID:15323564] |
| ChEMBL | Affinity Phenotypic Cellular interaction: (Inhibition of IL-2 secretion (in murine EL4 cells)) EUB0000651a ITK | F | 7.14 | pIC50 | 72 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity Phenotypic Cellular interaction: (Dose-dependent inhibition of calcium mobilization) EUB0000651a ITK | F | 7.28 | pIC50 | 52 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| GtoPdb | - | - | 7.72 | pIC50 | 19 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 3706-12 [PMID:16682193] |
| ChEMBL | Selectivity interaction (Kinase panel (radiometric inhibition assay)) EUB0000651a ITK | B | 7.72 | pIC50 | 19 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Inhibition of human Itk using GST-SLP-76 as peptide substrate incubated for 10 mins in presence of [gamma-33P]ATP by scintillation counter assay | B | 7.72 | pIC50 | 19 | nM | IC50 | Biochemistry (2004) 43: 11056-11062 [PMID:15323564] |
| ChEMBL | Affinity Biochemical interaction: (Enzymatic radiometric assay) EUB0000651a ITK | B | 7.72 | pIC50 | 19 | nM | IC50 | Affinity Biochemical Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Inhibition of Itk | B | 7.72 | pIC50 | 19 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 3706-3712 [PMID:16682193] |
| ChEMBL | Inhibition of ITK (unknown origin) | B | 7.72 | pIC50 | 19 | nM | IC50 | J Med Chem (2023) 66: 4979-4998 [PMID:36959108] |
| ChEMBL | Inhibition of human ITK using poly-Glu-Tyr (4:1) as substrate incubated for 1 hr by ELISA | B | 7.99 | pIC50 | 10.3 | nM | IC50 | J Med Chem (2022) 65: 2694-2709 [PMID:35099969] |
| IL2 inducible T cell kinase/Tyrosine-protein kinase ITK/TSK in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6067600] [GtoPdb: 2046] [UniProtKB: Q03526] | ||||||||
| ChEMBL | Inhibition of Itk in mouse Splenocyte cells assessed as inhibition of IL-2 secretion incubated for 16 hrs in presence of anti-CD3 antibody G19-4 by ELISA analysis | B | 6.42 | pIC50 | 380 | nM | IC50 | Biochemistry (2004) 43: 11056-11062 [PMID:15323564] |
| ChEMBL | Inhibition of Itk in mouse EL4 cells assessed as inhibition of IL-2 secretion incubated for 16 hrs in presence of anti-CD3 antibody G19-4 by ELISA analysis | B | 7.14 | pIC50 | 72 | nM | IC50 | Biochemistry (2004) 43: 11056-11062 [PMID:15323564] |
| LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lck in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239] | ||||||||
| ChEMBL | Inhibition of LCK | B | 5.62 | pIC50 | 2400 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 3706-3712 [PMID:16682193] |
| ChEMBL | Inhibition of Lck (unknown origin) using GST-SLP-76 as peptide substrate incubated for 10 mins in presence of [gamma-33P]ATP by scintillation counter assay | B | 5.62 | pIC50 | 2400 | nM | IC50 | Biochemistry (2004) 43: 11056-11062 [PMID:15323564] |
| spleen associated tyrosine kinase/Tyrosine-protein kinase SYK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2599] [GtoPdb: 2230] [UniProtKB: P43405] | ||||||||
| ChEMBL | Inhibition of Syk | B | 4.3 | pIC50 | >50000 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 3706-3712 [PMID:16682193] |
| ChEMBL | Selectivity interaction (Kinase panel (radiometric inhibition assay)) EUB0000651a SYK | B | 4.3 | pIC50 | >50000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Inhibition of Syk (unknown origin) using GST-SLP-76 as peptide substrate incubated for 10 mins in presence of [gamma-33P]ATP by scintillation counter assay | B | 4.3 | pIC50 | >50000 | nM | IC50 | Biochemistry (2004) 43: 11056-11062 [PMID:15323564] |
| tec protein tyrosine kinase/Tyrosine-protein kinase Tec in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4246] [GtoPdb: 2238] [UniProtKB: P42680] | ||||||||
| ChEMBL | Inhibition of Tec | B | 4.77 | pIC50 | 17000 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 3706-3712 [PMID:16682193] |
| ChEMBL | Selectivity interaction (Kinase panel (radiometric inhibition assay)) EUB0000651a TEC | B | 4.77 | pIC50 | 17000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Inhibition of Tec (unknown origin) using GST-SLP-76 as peptide substrate incubated for 10 mins in presence of [gamma-33P]ATP by scintillation counter assay | B | 4.77 | pIC50 | 17000 | nM | IC50 | Biochemistry (2004) 43: 11056-11062 [PMID:15323564] |
| TXK tyrosine kinase/Tyrosine-protein kinase TXK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4367] [GtoPdb: 2268] [UniProtKB: P42681] | ||||||||
| ChEMBL | Inhibition of Txk | B | 4.96 | pIC50 | 11000 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 3706-3712 [PMID:16682193] |
| ChEMBL | Selectivity interaction (Kinase panel (radiometric inhibition assay)) EUB0000651a TXK | B | 4.96 | pIC50 | 11000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Inhibition of Txk (unknown origin) using GST-SLP-76 as peptide substrate incubated for 10 mins in presence of [gamma-33P]ATP by scintillation counter assay | B | 4.96 | pIC50 | 11000 | nM | IC50 | Biochemistry (2004) 43: 11056-11062 [PMID:15323564] |
| zeta chain of T cell receptor associated protein kinase 70/Tyrosine-protein kinase ZAP-70 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2803] [GtoPdb: 2285] [UniProtKB: P43403] | ||||||||
| ChEMBL | Inhibition of ZAP70 | B | 4.3 | pIC50 | >50000 | nM | IC50 | Bioorg Med Chem Lett (2006) 16: 3706-3712 [PMID:16682193] |
| ChEMBL | Selectivity interaction (Kinase panel (radiometric inhibition assay)) EUB0000651a ZAP70 | B | 4.3 | pIC50 | >50000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Inhibition of ZAP-70 (unknown origin) using GST-SLP-76 as peptide substrate incubated for 10 mins in presence of [gamma-33P]ATP by scintillation counter assay | B | 4.3 | pIC50 | >50000 | nM | IC50 | Biochemistry (2004) 43: 11056-11062 [PMID:15323564] |
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]
