Table 1 Effect of BI-D1870 on 54 protein kinases

Results are presented as percentage of kinase activity relative to control assays (without BI-D1870). Protein kinases were assayed as described in the Supplementary section (at http://www.BiochemJ.org/bj/401/bj4010029add.htm), in the absence or presence of the indicated amount of BI-D1870. As ATP concentrations can affect the apparent IC50 value of ATP-competitive inhibitors, assays were undertaken at the approximate Km concentration of ATP, namely 5 μM for p38δ, PKBα, GSK3β, p38γ, CK2, ERK8, MKK1, PIM2, IKKβ, PRK2, MARK3, EF2K and PLK1; 20 μM for JNK1, PRAK, ROCK-II, P38β2, CDK2, CHK1, CHK2, MSK1, CSK, S6K1, PKA, CK1, MAPKAP-K2, SGK1, PKCα, PDK1, NEK7, MAPKAP-K3, Aurora B and MST2; and 50 μM for p38α, Lck, AMPK, ERK2, DYRK1a, PHK, RSK1, RSK2, NEK6, NEK2a, CaMK-1, PKD1, SRPK-1, JNK3, MNK1, MNK2, Src, PKBβ and smMLCK). Results are means±S.D. of triplicates. Abbreviations not defined in main text: AMPK, AMP-activated protein kinase; CaMK-1, Ca2+/calmodulin-dependent kinase 1; CHK1, cell cycle checkpoint kinase-1; CSK, C-terminal Src kinase; EF2K, elongation factor 2 kinase; MARK3, microtubule affinity regulating kinase 3; M-K2, MAPK-activated protein kinase-2; MNK, MAPK interacting kinase; MST2, mammalian sterile 20-like 2; NEK, NIMA-related protein kinase; PHK, phosphorylase kinase; PKD1, protein kinase D1; PRAK, p38-regulated/activated protein kinase; PRK2, PKC-related kinase-2; smMLCK, smooth-muscle light-chain kinase; SRPK1, serine/arginine protein kinase 1. Kinase families are defined as in [42].

BI-D1870
10 μM0.1 μM10 nM
Protein kinaseKinase family% Remaining kinase activity
RSK1AGC3±01±115±3
RSK2AGC2±12±032±3
RSK3AGC1±113±265±6
RSK4AGC1±112±355±5
MSK1AGC71±787±295±5
PKBαAGC95±8116±12110±5
PKBβAGC95±797±1100±4
S6K1AGC54±268±183±4
SGK1AGC67±1183±499±3
PKCαAGC37±642±2103±5
PKAAGC66±694±291±4
PDK1AGC79±786±199±4
ROCKIIAGC70±480±0104±2
PRK2AGC68±672±180±6
MKK1STE49±176±2103±4
MST2STE13±149±465±8
JNK1CMGC83±987±698±5
JNK3CMGC72±176±095±5
p38αCMGC77±1186±689±3
p38β2CMGC91±986±290±0
p38γCMGC89±493±599±9
p38δCMGC89±086±689±1
ERK2CMGC74±086±196±2
ERK8CMGC54±8110±494±1
GSK3βCMGC21±329±384±0
CDK2–ACMGC30±738±1089±5
DYRK1aCMGC46±657±591±3
SRPK1CMGC80±1087±398±2
M-K2CaMK90±898±1093±6
M-K3CaMK92±499±158±5
CaMK-1CaMK60±967±494±5
smMLCKCaMK46±667±1106±4
MARK3CaMK37±239±4101±1
PKD1CaMK53±549±390±6
AMPKCaMK68±270±2101±3
CHK1CaMK74±788±999±8
CHK2CaMK65±279±297±9
PHKCaMK100±5104±277±2
MNK1CaMK76±080±098±6
MNK2CaMK86±492±1122±4
PRAKCaMK74±574±585±8
PIM2CaMK61±471±099±5
CK1CK132±051±394±0
CK2CK1100±395±0101±3
EF2Katypical96±1101±0108±3
NEK2aNEK81±087±094±5
NEK6NEK92±1100±189±4
NEK7NEK76±483±12107±9
IKKβIKK75±483±695±5
Aurora BAurora5±042±454±6
PLK1PLK15±217±133±1
LckTK35±245±190±3
CSKTK81±1292±791±2
SrcTK60±469±098±2