JNJ-28312141 [Ligand Id: 5689] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1908842 (JNJ-28312141) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| bone morphogenetic protein receptor type 2/Bone morphogenetic protein receptor type-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5467] [GtoPdb: 1794] [UniProtKB: Q13873] | ||||||||
| ChEMBL | Inhibition of BMPR2 (unknown origin) assessed as dissociation constant | B | 6.51 | pKd | 310 | nM | Kd | ACS Med Chem Lett (2023) 14: 833-840 [PMID:37312836] |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Displacement of [3H]astemizole from human ERG potassium channel | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2011) 54: 7860-7883 [PMID:22039836] |
| colony stimulating factor 1 receptor in Human [GtoPdb: 1806] [UniProtKB: P07333] | ||||||||
| GtoPdb | - | - | 8.49 | pKd | 3.2 | nM | Kd | Nat Biotechnol (2011) 29: 1046-51 [PMID:22037378] |
| GtoPdb | - | - | 9.16 | pIC50 | 0.69 | nM | IC50 | Mol Cancer Ther (2009) 8: 3151-61 [PMID:19887542] |
| colony stimulating factor 1 receptor/Macrophage colony-stimulating factor 1 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5570] [GtoPdb: 1806] [UniProtKB: P09581] | ||||||||
| ChEMBL | Inhibition of FMS-mediated proliferation in CSF1-stimulated bone marrow-derived mouse macrophages assessed as inhibition of incorporation of bromodeoxyuridine into the DNA after 30 hrs by ELISA | B | 8.59 | pIC50 | 2.6 | nM | IC50 | J Med Chem (2011) 54: 7860-7883 [PMID:22039836] |
| colony stimulating factor 1 receptor/Macrophage colony stimulating factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1844] [GtoPdb: 1806] [UniProtKB: P07333] | ||||||||
| GtoPdb | - | - | 8.49 | pKd | 3.2 | nM | Kd | Nat Biotechnol (2011) 29: 1046-51 [PMID:22037378] |
| GtoPdb | - | - | 9.16 | pIC50 | 0.69 | nM | IC50 | Mol Cancer Ther (2009) 8: 3151-61 [PMID:19887542] |
| ChEMBL | Inhibition of FMS mediated phosphorylation using SYEGNSYTFIDPTQ as substrate after 80 mins by fluorescence polarization | B | 9.16 | pIC50 | 0.69 | nM | IC50 | J Med Chem (2011) 54: 7860-7883 [PMID:22039836] |
| ChEMBL | Inhibition of FMS | B | 9.16 | pIC50 | 0.69 | nM | IC50 | J Med Chem (2011) 54: 7860-7883 [PMID:22039836] |
| neurotrophic receptor tyrosine kinase 1/Nerve growth factor receptor Trk-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2815] [GtoPdb: 1817] [UniProtKB: P04629] | ||||||||
| ChEMBL | Inhibition of TRKA in human TF1 cells assessed as inhibition of NGF-induced cell proliferation after 72 hrs by CellTiter-Glo assay | B | 6.82 | pIC50 | 150 | nM | IC50 | J Med Chem (2011) 54: 7860-7883 [PMID:22039836] |
| GtoPdb | - | - | 7.82 | pIC50 | 15 | nM | IC50 | Mol Cancer Ther (2009) 8: 3151-61 [PMID:19887542] |
| ChEMBL | Inhibition of TRKA | B | 7.82 | pIC50 | 15 | nM | IC50 | J Med Chem (2011) 54: 7860-7883 [PMID:22039836] |
| receptor interacting serine/threonine kinase 1/Receptor-interacting serine/threonine-protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5464] [GtoPdb: 2189] [UniProtKB: Q13546] | ||||||||
| ChEMBL | Binding affinity to RIPK1 (unknown origin) | B | 6.62 | pKd | 240 | nM | Kd | J Med Chem (2022) 65: 14971-14999 [PMID:36346971] |
| RIO kinase 3/Serine/threonine-protein kinase RIO3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5659] [GtoPdb: 2188] [UniProtKB: O14730] | ||||||||
| ChEMBL | Binding affinity to RIOK3 (unknown origin) | B | 5.7 | pKd | 2000 | nM | Kd | US-20200216545-A1. Compositions and methods for treating beta-globinopathies (2020) |
| ChEMBL | Binding affinity to RIOK3 (unknown origin) | B | 5.7 | pKd | 1995.26 | nM | Kd | US-20200216545-A1. Compositions and methods for treating beta-globinopathies (2020) |
| KIT proto-oncogene, receptor tyrosine kinase/Stem cell growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1936] [GtoPdb: 1805] [UniProtKB: P10721] | ||||||||
| ChEMBL | Inhibition of KIT in human Mo7e cells assessed as inhibition of SCF-induced cell proliferation after 72 hrs by CellTiter-Glo assay | B | 7.39 | pIC50 | 41 | nM | IC50 | J Med Chem (2011) 54: 7860-7883 [PMID:22039836] |
| GtoPdb | - | - | 8.3 | pIC50 | 5 | nM | IC50 | Mol Cancer Ther (2009) 8: 3151-61 [PMID:19887542] |
| ChEMBL | Inhibition of KIT | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2011) 54: 7860-7883 [PMID:22039836] |
| 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 in human Jurkat cells assessed as inhibition of PMA and antiCD3-induced IL2 secretion after 24 hrs by ELISA | B | 5.41 | pIC50 | 3900 | nM | IC50 | J Med Chem (2011) 54: 7860-7883 [PMID:22039836] |
| ChEMBL | Inhibition of LCK | B | 7.06 | pIC50 | 88 | nM | IC50 | J Med Chem (2011) 54: 7860-7883 [PMID:22039836] |
| GtoPdb | - | - | 7.06 | pIC50 | 88 | nM | IC50 | Mol Cancer Ther (2009) 8: 3151-61 [PMID:19887542] |
| fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888] | ||||||||
| GtoPdb | - | - | 7.52 | pIC50 | 30 | nM | IC50 | Mol Cancer Ther (2009) 8: 3151-61 [PMID:19887542] |
| ChEMBL | Inhibition of FLT3 | B | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (2011) 54: 7860-7883 [PMID:22039836] |
| ChEMBL | Inhibition of FLT3 in human MV411 cells assessed as inhibition of cell proliferation after 72 hrs by CellTiter-Glo assay | B | 7.68 | pIC50 | 21 | nM | IC50 | J Med Chem (2011) 54: 7860-7883 [PMID:22039836] |
| AXL receptor tyrosine kinase/Tyrosine-protein kinase receptor UFO in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4895] [GtoPdb: 1835] [UniProtKB: P30530] | ||||||||
| ChEMBL | Inhibition of AXL overexpressed in human HEK cells assessed as inhibition of GAS6-induced autophosphorylation by immunoblot assay | B | 5.59 | pIC50 | 2600 | nM | IC50 | J Med Chem (2011) 54: 7860-7883 [PMID:22039836] |
| ChEMBL | Inhibition of AXL | B | 7.92 | pIC50 | 12 | nM | IC50 | J Med Chem (2011) 54: 7860-7883 [PMID:22039836] |
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]
