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Kinase inhibitor pathways

Inhibitors of ATM:

Name  C*  KS* Signature [GI50, log10(M)]
CP466722 T ✔
KU-55933 T
KU-60019 T

*  C = classification (Approved/Investigational/Tool);
KS = KinomeScan profile available (links to dataset)

Inhibitors of AKT (AKT1, AKT2, AKT3):

Name  C*  KS* Signature [GI50, log10(M)] **
A443654 T ✔
AT-7867 T
GSK690693 I
KIN001-102 T ✔
MK2206 I
Triciribine I
Cell lines:
BT-474 HCC1187 HCC1428
HCC38 HCC70 SK-BR-3

*  C = classification (Approved/Investigational/Tool);
KS = KinomeScan profile available (links to dataset)

** Data from Heiser et. al 2012

Inhibitors of PARP (PARP, PARP-2):

Name  C*  KS* Signature [GI50, log10(M)]
Olaparib I
Veliparib I

*  C = classification (Approved/Investigational/Tool);
KS = KinomeScan profile available (links to dataset)

Inhibitors of MDM2:

Name  C*  KS* Signature [GI50, log10(M)] **
Nutlin 3a T
Cell lines:
BT-474 HCC1187 HCC1428
HCC38 HCC70 SK-BR-3

*  C = classification (Approved/Investigational/Tool);
KS = KinomeScan profile available (links to dataset)

** Data from Heiser et. al 2012

Inhibitors of p90RSK:

Name  C*  KS* Signature [GI50, log10(M)]
Fmk T

*  C = classification (Approved/Investigational/Tool);
KS = KinomeScan profile available (links to dataset)

Inhibitors of Raf (B-Raf, C-Raf):

Name  C*  KS* Signature [GI50, log10(M)] **
AZ-628 T ✔
GDC-0879 T
GW-5074 T ✔
HG-6-64-01 T ✔
L-779450 T
PLX-4720 T ✔
R7204 A ✔
RAF 265 I
SB 590885 T ✔
Sorafenib A ✔
Cell lines:
BT-474 HCC1187 HCC1428
HCC38 HCC70 SK-BR-3

*  C = classification (Approved/Investigational/Tool);
KS = KinomeScan profile available (links to dataset)

** Data from Heiser et. al 2012

Inhibitors of FAK:

Name  C*  KS* Signature [GI50, log10(M)]
PF-431396 T
PF-562271 T
PF-573228 T

*  C = classification (Approved/Investigational/Tool);
KS = KinomeScan profile available (links to dataset)

Inhibitors of DNA-PK:

Name  C*  KS* Signature [GI50, log10(M)]
NU7441 T ✔
PI103 T
QL-X-138 T ✔
SAR245409 I
Torin2 T ✔

*  C = classification (Approved/Investigational/Tool);
KS = KinomeScan profile available (links to dataset)

Inhibitors of PKC:

Name  C*  KS* Signature [GI50, log10(M)]
Chelerythrine T
Enzastaurin I

*  C = classification (Approved/Investigational/Tool);
KS = KinomeScan profile available (links to dataset)

Inhibitors of CSF1R:

Name  C*  KS* Signature [GI50, log10(M)]
HG-6-64-01 T ✔
KIN001-269 T
Ki20227 T
WZ-4-145 T ✔
WZ-7043 T ✔

*  C = classification (Approved/Investigational/Tool);
KS = KinomeScan profile available (links to dataset)

Inhibitors of p38 (p38-alpha, p38-beta, p38-delta, p38-gamma):

Name  C*  KS* Signature [GI50, log10(M)]
BIRB 796 T
HG-6-64-01 T ✔
SB 203580 T
SB 239063 T
TAK-715 T ✔
VX-745 T

*  C = classification (Approved/Investigational/Tool);
KS = KinomeScan profile available (links to dataset)

Inhibitors of CHK1/2 (CHK1, CHK2):

Name  C*  KS* Signature [GI50, log10(M)] **
AZD-7762 I ✔
PF-477736 T
TCS 2312 T
Cell lines:
BT-474 HCC1187 HCC1428
HCC38 HCC70 SK-BR-3

*  C = classification (Approved/Investigational/Tool);
KS = KinomeScan profile available (links to dataset)

** Data from Heiser et. al 2012

Inhibitors of MEK5:

Name  C*  KS* Signature [GI50, log10(M)]
BIX 02189 T

*  C = classification (Approved/Investigational/Tool);
KS = KinomeScan profile available (links to dataset)

Inhibitors of Wee1:

Name  C*  KS* Signature [GI50, log10(M)]
MK1775 I

*  C = classification (Approved/Investigational/Tool);
KS = KinomeScan profile available (links to dataset)

Inhibitors of ERBB2:

Name  C*  KS* Signature [GI50, log10(M)] **
Afatinib I
CP724714 T ✔
Lapatinib A
Neratinib I ✔
Cell lines:
BT-474 HCC1187 HCC1428
HCC38 HCC70 SK-BR-3

*  C = classification (Approved/Investigational/Tool);
KS = KinomeScan profile available (links to dataset)

** Data from Heiser et. al 2012

Inhibitors of Src:

Name  C*  KS* Signature [GI50, log10(M)] **
Bosutinib A
Dasatinib A
Saracatinib I
WH-4-025 T ✔
XMD16-144 T ✔
Cell lines:
BT-474 HCC1187 HCC1428
HCC38 HCC70 SK-BR-3

*  C = classification (Approved/Investigational/Tool);
KS = KinomeScan profile available (links to dataset)

** Data from Heiser et. al 2012

Inhibitors of IGF1R:

Name  C*  KS* Signature [GI50, log10(M)] **
AEW541 T
AG1024 T
GSK1838705 T
GSK1904529A T
OSI-906 I
Cell lines:
BT-474 HCC1187 HCC1428
HCC38 HCC70 SK-BR-3

*  C = classification (Approved/Investigational/Tool);
KS = KinomeScan profile available (links to dataset)

** Data from Heiser et. al 2012

Inhibitors of HSP90 (HSP90 alpha, HSP90 beta):

Name  C*  KS* Signature [GI50, log10(M)] **
17-AAG T
Geldanamycin T
NVP-AUY922 T
Cell lines:
BT-474 HCC1187 HCC1428
HCC38 HCC70 SK-BR-3

*  C = classification (Approved/Investigational/Tool);
KS = KinomeScan profile available (links to dataset)

** Data from Heiser et. al 2012

Inhibitors of PI3K (PI3K-alpha, PI3K-beta, PI3K-delta, PI3K-gamma):

Name  C*  KS* Signature [GI50, log10(M)] **
A66 T
AS-252424 T
AS-605240 T
AZD-6482 T ✔
BEZ235 I
BYL719 T
CAL-101 I
GDC-0941 T ✔
GDC-0980 T
GSK1059615 I ✔
GSK1487371 T
GSK2119563 T
GSK2126458 I ✔
NVP-BKM120 I
SAR245408 I
SAR245409 I
TGX221 T
Torin2 T ✔
ZSTK474 I
Cell lines:
BT-474 HCC1187 HCC1428
HCC38 HCC70 SK-BR-3

*  C = classification (Approved/Investigational/Tool);
KS = KinomeScan profile available (links to dataset)

** Data from Heiser et. al 2012

Inhibitors of mTOR:

Name  C*  KS* Signature [GI50, log10(M)] **
AZD-8055 I
GDC-0980 T
GSK1059615 I ✔
GSK2126458 I ✔
OSI-027 T
QL-X-138 T ✔
RAD001 T
SAR245409 I
Sirolimus A
Temsirolimus A
Torin1 T ✔
Torin2 T ✔
WYE-125132 T ✔
Cell lines:
BT-474 HCC1187 HCC1428
HCC38 HCC70 SK-BR-3

*  C = classification (Approved/Investigational/Tool);
KS = KinomeScan profile available (links to dataset)

** Data from Heiser et. al 2012

Inhibitors of JAK (JAK1, JAK2, JAK3):

Name  C*  KS* Signature [GI50, log10(M)]
AZD-1480 I
CYT387 I ✔
KIN001-055 T
QL-X-138 T ✔
Ruxolitinib A
TG 101348 I

*  C = classification (Approved/Investigational/Tool);
KS = KinomeScan profile available (links to dataset)

Inhibitors of MEK1/2 (MEK1, MEK2):

Name  C*  KS* Signature [GI50, log10(M)] **
ARRY-424704 I
BMS-777607 I
CI-1040 T
GSK1120212 I
PD-325901 I ✔
PD-98059 T
Selumetinib I
Cell lines:
BT-474 HCC1187 HCC1428
HCC38 HCC70 SK-BR-3

*  C = classification (Approved/Investigational/Tool);
KS = KinomeScan profile available (links to dataset)

** Data from Heiser et. al 2012

Inhibitors of c-Met:

Name  C*  KS* Signature [GI50, log10(M)]
Amuvatinib I
Cabozantinib I
Crizotinib A ✔
Foretinib I
JNJ38877605 I
KIN001-237 T
MGCD265 I
PF-04217903 I
PHA-665752 T
PKI-SU11274 T
SGX523 I
Tivantinib I

*  C = classification (Approved/Investigational/Tool);
KS = KinomeScan profile available (links to dataset)

Inhibitors of ALK (ALK2, ALK3, ALK5):

Name  C*  KS* Signature [GI50, log10(M)] **
CH5424802 I
D 4476 T
GSK1838705 T
LDN-193189 T
NVP-TAE684 T
SB 525334 T
Cell lines:
BT-474 HCC1187 HCC1428
HCC38 HCC70 SK-BR-3

*  C = classification (Approved/Investigational/Tool);
KS = KinomeScan profile available (links to dataset)

** Data from Heiser et. al 2012

Inhibitors of JNK (JNK1, JNK2, JNK3):

Name  C*  KS* Signature [GI50, log10(M)] **
AS-601245 T ✔
CC-401 I
CG-930 T
JNK-9L T ✔
JNK-IN-5A T ✔
SP600125 T
ZG-10 T ✔
Cell lines:
BT-474 HCC1187 HCC1428
HCC38 HCC70 SK-BR-3

*  C = classification (Approved/Investigational/Tool);
KS = KinomeScan profile available (links to dataset)

** Data from Heiser et. al 2012

Inhibitors of p53:

Name  C*  KS* Signature [GI50, log10(M)]
JNJ26854165 I

*  C = classification (Approved/Investigational/Tool);
KS = KinomeScan profile available (links to dataset)

Inhibitors of PLK (PLK1, PLK2, PLK3):

Name  C*  KS* Signature [GI50, log10(M)] **
BI-2536 I ✔
GSK461364 I ✔
GW843682 T ✔
HMN-214 T
NPK76-II-72-1 T ✔
ON-01910 I
Cell lines:
BT-474 HCC1187 HCC1428
HCC38 HCC70 SK-BR-3

*  C = classification (Approved/Investigational/Tool);
KS = KinomeScan profile available (links to dataset)

** Data from Heiser et. al 2012

Inhibitors of c-Abl (c-Abl, Bcr-Abl):

Name  C*  KS* Signature [GI50, log10(M)]
GNF2 T
HG-5-113-01 T ✔
HG-6-64-01 T ✔
Imatinib A
Nilotinib A
Ponatinib I

*  C = classification (Approved/Investigational/Tool);
KS = KinomeScan profile available (links to dataset)

Inhibitors of Aurora (AURKA, AURKB, AURKC):

Name  C*  KS* Signature [GI50, log10(M)] **
Barasertib I ✔
GSK1070916 T
JWE-035 T ✔
KIN001-220 T ✔
MLN8054 T ✔
Tozasertib I
XMD16-144 T ✔
ZM-447439 T ✔
Cell lines:
BT-474 HCC1187 HCC1428
HCC38 HCC70 SK-BR-3

*  C = classification (Approved/Investigational/Tool);
KS = KinomeScan profile available (links to dataset)

** Data from Heiser et. al 2012

Inhibitors of EGFR:

Name  C*  KS* Signature [GI50, log10(M)] **
Afatinib I
Canertinib I
Erlotinib A
Gefitinib A
HG-5-88-01 T ✔
HG-6-64-01 T ✔
Lapatinib A
Pelitinib I
Tyrphostin T ✔
WZ-4-145 T ✔
WZ-4002 T ✔
Cell lines:
BT-474 HCC1187 HCC1428
HCC38 HCC70 SK-BR-3

*  C = classification (Approved/Investigational/Tool);
KS = KinomeScan profile available (links to dataset)

** Data from Heiser et. al 2012

Inhibitors of AMPK (AMPK-alpha1, AMPK-alpha2):

Name  C*  KS* Signature [GI50, log10(M)]
A769662 T

*  C = classification (Approved/Investigational/Tool);
KS = KinomeScan profile available (links to dataset)

Inhibitors of CDK (CDK1, CDK2, CDK4, CDK5, CDK6, CDK7, CDK9):

Name  C*  KS* Signature [GI50, log10(M)] **
AT-7519 I
AZD-5438 I
BMS-387032 I
Fascaplysin T
Flavopiridol I
KIN001-270 T
MLS000911536 T ✔
NU6102 T
PD0332991 I ✔
PHA-793887 T
Purvalanol A T
Seliciclib I
Cell lines:
BT-474 HCC1187 HCC1428
HCC38 HCC70 SK-BR-3

*  C = classification (Approved/Investigational/Tool);
KS = KinomeScan profile available (links to dataset)

** Data from Heiser et. al 2012

Inhibitors of PDK1:

Name  C*  KS* Signature [GI50, log10(M)]
BX-912 T ✔
KIN001-244 T

*  C = classification (Approved/Investigational/Tool);
KS = KinomeScan profile available (links to dataset)

Inhibitors of Bcl-2:

Name  C*  KS* Signature [GI50, log10(M)]
ABT-737 I
Docetaxel A
Paclitaxel A

*  C = classification (Approved/Investigational/Tool);
KS = KinomeScan profile available (links to dataset)

Inhibitors of FLT3:

Name  C*  KS* Signature [GI50, log10(M)] **
AC220 I
Dovitinib I
HG-6-64-01 T ✔
KW2449 I
Lestaurtinib I
Linifanib I
Sunitinib A
WZ-3105 T ✔
Cell lines:
BT-474 HCC1187 HCC1428
HCC38 HCC70 SK-BR-3

*  C = classification (Approved/Investigational/Tool);
KS = KinomeScan profile available (links to dataset)

** Data from Heiser et. al 2012

Inhibitors of MNK (MNK1, MNK2):

Name  C*  KS* Signature [GI50, log10(M)]
QL-X-138 T ✔

*  C = classification (Approved/Investigational/Tool);
KS = KinomeScan profile available (links to dataset)

Inhibitors of ERK5:

Name  C*  KS* Signature [GI50, log10(M)]
LRRK2-in-1 T ✔
XMD8-85 T ✔
XMD8-92 T ✔

*  C = classification (Approved/Investigational/Tool);
KS = KinomeScan profile available (links to dataset)

Inhibitors of GSK3 (GSK3A, GSK3B):

Name  C*  KS* Signature [GI50, log10(M)]
CHIR-99021 T
KIN001-042 T
KIN001-043 T
SB 216763 T
TWS119 T

*  C = classification (Approved/Investigational/Tool);
KS = KinomeScan profile available (links to dataset)

Inhibitors of FGFR (FGFR1, FGFR3):

Name  C*  KS* Signature [GI50, log10(M)] **
BGJ398 I
HG-6-64-01 T ✔
PD-173074 T ✔
Vargatef I
WZ-7043 T ✔
Cell lines:
BT-474 HCC1187 HCC1428
HCC38 HCC70 SK-BR-3

*  C = classification (Approved/Investigational/Tool);
KS = KinomeScan profile available (links to dataset)

** Data from Heiser et. al 2012

Inhibitors of EPHB3:

Name  C*  KS* Signature [GI50, log10(M)]
XMD14-99 T ✔

*  C = classification (Approved/Investigational/Tool);
KS = KinomeScan profile available (links to dataset)

Inhibitors of IKK (IKK-alpha, IKK-beta, IKK-epsilon):

Name  C*  KS* Signature [GI50, log10(M)] **
BMS-345541 T ✔
TPCA-1 T
Cell lines:
BT-474 HCC1187 HCC1428
HCC38 HCC70 SK-BR-3

*  C = classification (Approved/Investigational/Tool);
KS = KinomeScan profile available (links to dataset)

** Data from Heiser et. al 2012

Inhibitors of c-Kit:

Name  C*  KS* Signature [GI50, log10(M)] **
Amuvatinib I
HG-6-64-01 T ✔
Masitinib I
OSI-930 I
Sunitinib A
Cell lines:
BT-474 HCC1187 HCC1428
HCC38 HCC70 SK-BR-3

*  C = classification (Approved/Investigational/Tool);
KS = KinomeScan profile available (links to dataset)

** Data from Heiser et. al 2012

Inhibitors of DDR1:

Name  C*  KS* Signature [GI50, log10(M)]
ALW-II-38-3 T ✔
ALW-II-49-7 T ✔
QL-XI-92 T ✔
WZ-4-145 T ✔
WZ-7043 T ✔

*  C = classification (Approved/Investigational/Tool);
KS = KinomeScan profile available (links to dataset)

Inhibitors of ERK1/2 (ERK1, ERK2):

Name  C*  KS* Signature [GI50, log10(M)]
FR180204 T

*  C = classification (Approved/Investigational/Tool);
KS = KinomeScan profile available (links to dataset)

One component of the HMS LINCS initiative is the creation of a highly curated library of kinase inhibitors. We are focusing on clinical compounds (FDA approved or undergoing trials) and tool compounds which are highly selective for important kinases.

This network map of key signal transduction pathways includes the majority of kinases we can selectively target with small molecules, as well as information on the relevant inhibitors in the HMS LINCS library. This allows biologists to find compounds which target a given kinase or affect a specific phenotypic outcome, as well as to identify compounds with potentially similar or synergistic effects by virtue of targeting different nodes in the same signal transduction cascade.

Instructions

Hover or tap on a kinase shaded in orange to view a box listing compounds in the HMS LINCS library which inhibit the activity of that kinase. For each compound, the box shows the following summary information: the inhibitor's classification (Approved/Investigational/Tool - see below), a link to a KinomeScan profile of the compound (if available), and a graphical visualization of the compound's ability to inhibit growth of a panel of six breast cancer cell lines (data from Heiser et. al 2012). Protein, compound and cell line names are all hyperlinked to entries in the HMS LINCS Database which contain detailed information.

Compound classifications:

  • Approved: FDA approved for use in human subjects
  • Investigational: Undergoing clinical trials
  • Tool: Only suitable for research in cell culture

You may also use our full database search engine to find compounds or protein targets by name or other attributes.

References

  1. Heiser, L. et al. (2012) Subtype and pathway specific responses to anticancer compounds in breast cancer. Proc Natl Acad Sci. 109(8), 2724-9. doi:10.1073/pnas.1018854108 PMID:22003129 PMCID:PMC3286973