Ki Summary

Reaction Details

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Target

Serine/threonine-protein kinase N1

Ligand

BDBM106870

Substrate/Competitor

n/a

Meas. Tech.

ChEMBL_1544403 (CHEMBL3749781)

IC50

4900±n/a nM

Citation

Burger, MT; Nishiguchi, G; Han, W; Lan, J; Simmons, R; Atallah, G; Ding, Y; Tamez, V; Zhang, Y; Mathur, M; Muller, K; Bellamacina, C; Lindvall, MK; Zang, R; Huh, K; Feucht, P; Zavorotinskaya, T; Dai, Y; Basham, S; Chan, J; Ginn, E; Aycinena, A; Holash, J; Castillo, J; Langowski, JL; Wang, Y; Chen, MY; Lambert, A; Fritsch, C; Kauffmann, A; Pfister, E; Vanasse, KG; Garcia, PD Identification of N-(4-((1R,3S,5S)-3-Amino-5-methylcyclohexyl)pyridin-3-yl)-6-(2,6-difluorophenyl)-5-fluoropicolinamide (PIM447), a Potent and Selective Proviral Insertion Site of Moloney Murine Leukemia (PIM) 1, 2, and 3 Kinase Inhibitor in Clinical Trials for Hematological Malignancies. J Med Chem58:8373-86 (2015) [PubMed] Article

More Info.:

Get all data from this article, Assay Method

Serine/threonine-protein kinase N1

Name:

Serine/threonine-protein kinase N1

Synonyms:

PAK1 | PKN | PKN1 | PKN1_HUMAN | PRK1 | PRKCL1 | Protein kinase N1 | Serine/threonine-protein kinase N1/Transforming protein RhoA

Type:

PROTEIN

Mol. Mass.:

103928.39

Organism:

Homo sapiens (Human)

Description:

ChEMBL_1433150

Residue:

942

Sequence:

MASDAVQSEPRSWSLLEQLGLAGADLAAPGVQQQLELERERLRREIRKELKLKEGAENLR
RATTDLGRSLGPVELLLRGSSRRLDLLHQQLQELHAHVVLPDPAATHDGPQSPGAGGPTC
SATNLSRVAGLEKQLAIELKVKQGAENMIQTYSNGSTKDRKLLLTAQQMLQDSKTKIDII
RMQLRRALQAGQLENQAAPDDTQGSPDLGAVELRIEELRHHFRVEHAVAEGAKNVLRLLS
AAKAPDRKAVSEAQEKLTESNQKLGLLREALERRLGELPADHPKGRLLREELAAASSAAF
STRLAGPFPATHYSTLCKPAPLTGTLEVRVVGCRDLPETIPWNPTPSMGGPGTPDSRPPF
LSRPARGLYSRSGSLSGRSSLKAEAENTSEVSTVLKLDNTVVGQTSWKPCGPNAWDQSFT
LELERARELELAVFWRDQRGLCALKFLKLEDFLDNERHEVQLDMEPQGCLVAEVTFRNPV
IERIPRLRRQKKIFSKQQGKAFQRARQMNIDVATWVRLLRRLIPNATGTGTFSPGASPGS
EARTTGDISVEKLNLGTDSDSSPQKSSRDPPSSPSSLSSPIQESTAPELPSETQETPGPA
LCSPLRKSPLTLEDFKFLAVLGRGHFGKVLLSEFRPSGELFAIKALKKGDIVARDEVESL
MCEKRILAAVTSAGHPFLVNLFGCFQTPEHVCFVMEYSAGGDLMLHIHSDVFSEPRAIFY
SACVVLGLQFLHEHKIVYRDLKLDNLLLDTEGYVKIADFGLCKEGMGYGDRTSTFCGTPE
FLAPEVLTDTSYTRAVDWWGLGVLLYEMLVGESPFPGDDEEEVFDSIVNDEVRYPRFLSA
EAIGIMRRLLRRNPERRLGSSERDAEDVKKQPFFRTLGWEALLARRLPPPFVPTLSGRTD
VSNFDEEFTGEAPTLSPPRDARPLTAAEQAAFLDFDFVAGGC

BDBM106870

n/a

Name

BDBM106870

Synonyms:

US8592455, 70

Type

Small organic molecule

Emp. Form.

C24H23F3N4O

Mol. Mass.

440.4608

SMILES

C[C@@H]1C[C@H](N)C[C@@H](C1)c1ccncc1NC(=O)c1ccc(F)c(n1)-c1c(F)cccc1F |r,wU:6.8,3.3,1.0,(-.67,2.69,;-2,1.93,;-3.33,2.69,;-4.67,1.93,;-6,2.69,;-4.67,.38,;-3.33,-.38,;-2,.38,;-3.33,-1.93,;-4.67,-2.69,;-4.67,-4.23,;-3.33,-5,;-2,-4.23,;-2,-2.69,;-.67,-1.93,;.67,-2.69,;.67,-4.23,;2,-1.93,;3.33,-2.69,;4.67,-1.93,;4.67,-.38,;6,.38,;3.33,.38,;2,-.38,;3.33,1.93,;4.67,2.69,;6,1.93,;4.67,4.23,;3.33,5,;2,4.23,;2,2.69,;.67,1.93,)|

Structure