Reaction Details |
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Target | Mitogen-activated protein kinase kinase kinase kinase 1 |
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Ligand | BDBM591168 |
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Substrate/Competitor | n/a |
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Meas. Tech. | HPK1-FL HTRF Enzymatic Assay |
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Ki | 0.021±n/a nM |
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Citation | Chan, B; Drobnick, J; Gazzard, L; Heffron, T; Liang, J; Malhotra, S; Mendonca, R; Rajapaksa, N; Stivala, C; Tellis, J; Wang, W; Wei, B; Zhou, A; Cartwright, MW; Lainchbury, M; Gancia, E; Seward, E; Madin, A; Favor, D; Fong, KC; Hu, Y; Good, A Isoquinolines as inhibitors of HPK1 US Patent US11566003 Publication Date 1/31/2023 |
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More Info.: | Get all data from this article, Assay Method |
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Mitogen-activated protein kinase kinase kinase kinase 1 |
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Name: | Mitogen-activated protein kinase kinase kinase kinase 1 |
Synonyms: | HPK1 | M4K1_HUMAN | MAP4K1 |
Type: | PROTEIN |
Mol. Mass.: | 91316.07 |
Organism: | Homo sapiens (Human) |
Description: | ChEMBL_586597 |
Residue: | 833 |
Sequence: | MDVVDPDIFNRDPRDHYDLLQRLGGGTYGEVFKARDKVSGDLVALKMVKMEPDDDVSTLQ
KEILILKTCRHANIVAYHGSYLWLQKLWICMEFCGAGSLQDIYQVTGSLSELQISYVCRE
VLQGLAYLHSQKKIHRDIKGANILINDAGEVRLADFGISAQIGATLARRLSFIGTPYWMA
PEVAAVALKGGYNELCDIWSLGITAIELAELQPPLFDVHPLRVLFLMTKSGYQPPRLKEK
GKWSAAFHNFIKVTLTKSPKKRPSATKMLSHQLVSQPGLNRGLILDLLDKLKNPGKGPSI
GDIEDEEPELPPAIPRRIRSTHRSSSLGIPDADCCRRHMEFRKLRGMETRPPANTARLQP
PRDLRSSSPRKQLSESSDDDYDDVDIPTPAEDTPPPLPPKPKFRSPSDEGPGSMGDDGQL
SPGVLVRCASGPPPNSPRPGPPPSTSSPHLTAHSEPSLWNPPSRELDKPPLLPPKKEKMK
RKGCALLVKLFNGCPLRIHSTAAWTHPSTKDQHLLLGAEEGIFILNRNDQEATLEMLFPS
RTTWVYSINNVLMSLSGKTPHLYSHSILGLLERKETRAGNPIAHISPHRLLARKNMVSTK
IQDTKGCRACCVAEGASSGGPFLCGALETSVVLLQWYQPMNKFLLVRQVLFPLPTPLSVF
ALLTGPGSELPAVCIGVSPGRPGKSVLFHTVRFGALSCWLGEMSTEHRGPVQVTQVEEDM
VMVLMDGSVKLVTPEGSPVRGLRTPEIPMTEAVEAVAMVGGQLQAFWKHGVQVWALGSDQ
LLQELRDPTLTFRLLGSPRLECSGTISPHCNLLLPGSSNSPASASRVAGITGL
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BDBM591168 |
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n/a |
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Name | BDBM591168 |
Synonyms: | 2-((8-amino-6-(5-amino-4- methylpyridin-3-yl)-7-fluoroisoquinolin- 3-yl)amino)-5,5-dimethyl-5,6-dihydro- 4H-pyrazolo[1,5-d][1,4]diazepin-7(8H)- one | US11566003, Compound 234 |
Type | Small organic molecule |
Emp. Form. | C24H25FN8O |
Mol. Mass. | 460.5067 |
SMILES | Cc1c(N)cncc1-c1cc2cc(Nc3cc4CC(C)(C)NC(=O)Cn4n3)ncc2c(N)c1F |
Structure |
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