Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T37961 | Target Info | |||
| Target Name | PAK-1 protein kinase (PAK1) | ||||
| Synonyms |
p65-PAK; p21-activated kinase 1; Serine/threonine-protein kinase PAK 1; PAK-1; Alpha-PAK
Click to Show/Hide
|
||||
| Target Type | Literature-reported Target | ||||
| Gene Name | PAK1 | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 4 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
5-[[5-Chloro-4-[3-(cyanomethyl)phenyl]pyrimidin-2-yl]amino]-N,N-diethyl-2-(4-methylpiperazin-1-yl)benzamide
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2403073; BDBM50437032
Click to Show/Hide
|
||||
| Activity |
EC50 = 50100 nM
|
[1] | |||
| Compound Name |
2,8-Difluoro-11-(4-Methylpiperazin-1-Yl)-5h-Dibenzo[b,E][1,4]diazepine
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3609328; BDBM50112349; Q27454877
Click to Show/Hide
|
||||
| Activity |
IC50 = 54000 nM
|
[2] | |||
| Compound Name |
5-[[5-Chloro-4-[3-(cyanomethyl)phenyl]pyrimidin-2-yl]amino]-N-methyl-2-(4-methylpiperazin-1-yl)benzamide
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2403072; BDBM50437033
Click to Show/Hide
|
||||
| Activity |
EC50 = 61300 nM
|
[1] | |||
| Compound Name |
Chembl4276946
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
GTPL9965; compound 3a [Pipionne et al, 2018]; 1-[5-amino-4-(3,4-dichlorophenyl)-3-methyl-1H-pyrazol-1-yl]ethan-1-one
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[3] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Synthesis and structure-activity relationship of 2-arylamino-4-aryl-pyrimidines as potent PAK1 inhibitors. Bioorg Med Chem Lett. 2013 Jul 15;23(14):4072-5. | ||||
| REF 2 | Optimization of a Dibenzodiazepine Hit to a Potent and Selective Allosteric PAK1 Inhibitor. ACS Med Chem Lett. 2015 May 22;6(7):776-81. | ||||
| REF 3 | N-Acetyl-3-aminopyrazoles block the non-canonical NF-kB cascade by selectively inhibiting NIK. Medchemcomm. 2018 Apr 12;9(6):963-968. | ||||
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.