Co-Target(s) Information
| Target General Information | Top | ||||
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| Target ID | T40694 | Target Info | |||
| Target Name | Polo-like kinase 1 (PLK1) | ||||
| Synonyms |
Serine/threonine-protein kinase PLK1; Serine/threonine-protein kinase 13; Serine-threonine protein kinase 13; STPK13; Plk1; PLK-1; PLK; Mitoticserine-threonine kinase polo-like kinase 1
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| Target Type | Clinical trial Target | ||||
| Gene Name | PLK1 | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
|---|---|---|---|---|---|---|
| Co-Target Name | ALK tyrosine kinase receptor (ALK) | Successful Target | ||||
| UniProt ID | ALK_HUMAN | |||||
| Gene Name | ALK | |||||
| Synonyms |
CD246; Anaplastic lymphoma kinase
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| Representative Drug(s) | BI 2536 | Drug Info | IC50 = 180 nM | [1] | ||
| Co-Target Name | Fms-like tyrosine kinase 3 (FLT-3) | Successful Target | ||||
| UniProt ID | FLT3_HUMAN | |||||
| Gene Name | FLT3 | |||||
| Synonyms |
Stem cell tyrosine kinase 1; STK1; STK-1; Receptor-type tyrosine-protein kinase FLT3; Fetal liver kinase-2; FLT-3; FLK2; FLK-2; FL cytokine receptor; CD135
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| Representative Drug(s) | PCM-075 | Drug Info | IC50 = 510 nM | [2] | ||
| Co-Target Name | Bromodomain-containing protein 4 (BRD4) | Clinical trial Target | ||||
| UniProt ID | BRD4_HUMAN | |||||
| Gene Name | BRD4 | |||||
| Synonyms |
Protein HUNK1; HUNK1
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| Representative Drug(s) | BI 2536 | Drug Info | IC50 = 25 nM | [3] | ||
| Co-Target Name | Bromodomain testis-specific protein (BRDT) | Clinical trial Target | ||||
| UniProt ID | BRDT_HUMAN | |||||
| Gene Name | BRDT | |||||
| Synonyms |
Cancer/testis antigen 9; CT9
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| Representative Drug(s) | BI 2536 | Drug Info | IC50 = 260 nM | [4] | ||
| Co-Target Name | Maternal embryonic leucine zipper kinase (MELK) | Clinical trial Target | ||||
| UniProt ID | MELK_HUMAN | |||||
| Gene Name | MELK | |||||
| Synonyms |
Protein kinase PK38; Protein kinase Eg3
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| Representative Drug(s) | PCM-075 | Drug Info | IC50 = 744 nM | [2] | ||
| Co-Target Name | Polo-like kinase 2 (PLK2) | Patented-recorded Target | ||||
| UniProt ID | PLK2_HUMAN | |||||
| Gene Name | PLK2 | |||||
| Synonyms |
hSNK; hPlk2; Serum-inducible kinase; Serine/threonine-protein kinase SNK; Serine/threonine-protein kinase PLK2; SNK; PLK-2
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| Representative Drug(s) | BI 2536 | Drug Info | IC50 = 13.55 nM | [5] | ||
| Co-Target Name | Serine/threonine-protein kinase PLK3 (PLK3) | Co-Target | ||||
| UniProt ID | PLK3_HUMAN | |||||
| Gene Name | PLK3 | |||||
| Synonyms |
Cytokine-inducible serine/threonine-protein kinase; FGF-inducible kinase; Polo-like kinase 3; PLK-3; Proliferation-related kinase
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| Representative Drug(s) | BI 2536 | Drug Info | IC50 = 20.78 nM | [6] | ||
| Co-Target Name | Transcription initiation factor TFIID 1 (TAF1) | Co-Target | ||||
| UniProt ID | TAF1_HUMAN | |||||
| Gene Name | TAF1 | |||||
| Synonyms |
Transcription initiation factor TFIID subunit 1; Cell cycle gene 1 protein; TBP-associated factor 250 kDa; p250; Transcription initiation factor TFIID 250 kDa subunit; TAF(II)250; TAFII-250; TAFII250
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| Representative Drug(s) | BI 2536 | Drug Info | IC50 = 160 nM | [7] | ||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Designing Dual Inhibitors of Anaplastic Lymphoma Kinase (ALK) and Bromodomain-4 (BRD4) by Tuning Kinase Selectivity. J Med Chem. 2019 Mar 14;62(5):2618-2637. | ||||
| REF 2 | NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor. Bioorg Med Chem Lett. 2011 May 15;21(10):2969-74. | ||||
| REF 3 | Privileged Structures and Polypharmacology within and between Protein Families. ACS Med Chem Lett. 2018 Nov 16;9(12):1199-1204. | ||||
| REF 4 | Non-kinase targets of protein kinase inhibitors. Nat Rev Drug Discov. 2017 Jun;16(6):424-40. | ||||
| REF 5 | Design, synthesis, and biological evaluation of novel highly selective polo-like kinase 2 inhibitors based on the tetrahydropteridin chemical scaffold. Eur J Med Chem. 2018 Jan 1;143:724-31. | ||||
| REF 6 | Structure-based design and SAR development of novel selective polo-like kinase 1 inhibitors having the tetrahydropteridin scaffold. Eur J Med Chem. 2019 Dec 15;184:111769. | ||||
| REF 7 | Dual Inhibition of TAF1 and BET Bromodomains from the BI-2536 Kinase Inhibitor Scaffold. ACS Med Chem Lett. 2019 Sep 13;10(10):1443-1449. | ||||
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