Sequence: RecName: Full=Tyrosine-protein kinase ABL1; AltName: Full=Abelson murine leukemia viral oncogene homolog 1; AltName: Full=Abelson tyrosine-protein kinase 1; AltName: Full=Proto-oncogene c-Abl; AltName: Full=p150 Description ..    Breakpoint cluster region protein Protein Family: Catalytic domain of the Protein Tyrosine Kinase, Abelson kinase Comment ..    Confidence: Direct protein complex subunits assigned Gene Name: BCR;BCR1;D22S11 Pref Name: Bcr/Abl fusion protein Description: Breakpoint cluster region protein Synonyms: Breakpoint cluster region protein;Renal carcinoma antigen NY-REN-26 Db Source: SWISS-PROT Db Version: 2012_01 Relationship Type: Direct protein target assigned Target Class L1: Cytosolic other Target Classification: cytosolic other Target Class L1: Enzyme Target Class L2: Kinase Target Class L3: Protein Kinase Target Class L4: Ser_Thr Target Class L5: Atypical Target Class L6: Bcr Target Classification: enzyme kinase protein kinase ser_thr atypical bcr Target Class L1: Enzyme Target Class L2: Kinase Target Class L3: Protein Kinase Target Class L4: Tyr Target Class L5: Tk Target Class L6: Abl Target Classification: enzyme kinase protein kinase tyr tk abl Gene:ABL1     Related Protein 3D Structures

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Title: Identification of a terphenyl derivative that blocks the cell cycle in the G0-G1 phase and induces differentiation in leukemia cells.

Abstract: To further explore the SAR of resveratrol-related trans-stilbene derivatives, here we describe the synthesis of (a) a series of 3,5-dimethoxy analogues in which a variety of substituents were introduced at positions 2', 3', 4', and 5' of the stilbene scaffold and (b) a second group of derivatives (2-phenylnaphthalenes and terphenyls) that incorporate a phenyl ring as a bioisosteric replacement of the stilbene alkenyl bridge. We thoroughly characterized all of the new compounds with respect to their apoptosis-inducing activity and their effects on the cell cycle. One of the new derivatives, 13g, behaved differently from the others, as it was able to block the cell cycle in the G(0)-G(1) phase and also to induce differentiation in acute myelogenous leukemia HL60 cells. Compared to resveratrol, the synthetic terphenyl 13g showed a more potent apoptotic and differentiating activity. Moreover, it was active on both multidrug resistance and Bcr-Abl-expressing cells that were resistant to resveratrol.
(PMID: 16686543)

Compounds with activity <= 50uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.

ChEMBL Assay Type: Functional

ChEMBL Assay Data Source: Scientific Literature

ChEMBL Target ID: 104811

ChEMBL target type: NULL