DGIdb - CI-1040 Drug Record

CI-1040 chembl:CHEMBL105442 Antineoplastic

Alternate Names:

CI 1040
PD-184352
CI-1040
PD-18435

Drug Info:

Notes	allosteric inhibitor
Drug Class	Kinase Inhibitors

(2 More Sources)

Publications:

Delaney et al., 2002, Identification of a novel mitogen-activated protein kinase kinase activation domain recognized by the inhibitor PD 184352., Mol. Cell. Biol.
Emery et al., 2009, MEK1 mutations confer resistance to MEK and B-RAF inhibition., Proc. Natl. Acad. Sci. U.S.A.
Nakayama et al., 2008, KRAS or BRAF mutation status is a useful predictor of sensitivity to MEK inhibition in ovarian cancer., Br. J. Cancer
Whittaker et al., 2010, Gatekeeper mutations mediate resistance to BRAF-targeted therapies., Sci Transl Med
Kaufman et al., 2017, A Transcriptional Signature Identifies LKB1 Functional Status as a Novel Determinant of MEK Sensitivity in Lung Adenocarcinoma., Cancer Res.
Herrero et al., 2015, Small Molecule Inhibition of ERK Dimerization Prevents Tumorigenesis by RAS-ERK Pathway Oncogenes., Cancer Cell
Yeh et al., 2009, KRAS/BRAF mutation status and ERK1/2 activation as biomarkers for MEK1/2 inhibitor therapy in colorectal cancer., Mol. Cancer Ther.
Rexer et al., 2013, Human breast cancer cells harboring a gatekeeper T798M mutation in HER2 overexpress EGFR ligands and are sensitive to dual inhibition of EGFR and HER2., Clin. Cancer Res.
Li Q et al., 2010, Discovery of 3-(2-aminoethyl)-5-(3-phenyl-propylidene)-thiazolidine-2,4-dione as a dual inhibitor of the Raf/MEK/ERK and the PI3K/Akt signaling pathways., Bioorg Med Chem Lett

CI-1040 MAP3K2

Interaction Score: 2.69

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
CI-1040 RPS6KA1

Interaction Score: 1.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
20580230

Sources:
DTC
CI-1040 SGK1

Interaction Score: 0.9

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
CI-1040 MAP3K1

Interaction Score: 0.34

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
CI-1040 MAP2K1

Interaction Score: 0.27

Interaction Types & Directionality:

allosteric modulator

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type melanoma

Response Type resistant

Approval Status Preclinical - Cell culture

PMIDs:
12370306 19915144

Sources:
MyCancerGenome JAX-CKB ChemblInteractions
CI-1040 STK11

Interaction Score: 0.23

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Cell culture

Response Type sensitive

PMIDs:
27821489

Sources:
JAX-CKB
CI-1040 HRAS

Interaction Score: 0.16

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type melanoma

Response Type sensitive

Approval Status Preclinical

PMIDs:
26267534

Sources:
JAX-CKB
CI-1040 PRKCA

Interaction Score: 0.14

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
CI-1040 MAP2K2

Interaction Score: 0.13

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Dual specificity mitogen-activated protein kinase kinase 2 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
MyCancerGenome ChemblInteractions
CI-1040 MAPK11

Interaction Score: 0.12

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
CI-1040 BRAF

Interaction Score: 0.11

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type Advanced Solid Tumor

Response Type sensitive

Approval Status Preclinical

PMIDs:
19018267 19915144 20538618

Sources:
JAX-CKB
CI-1040 MAPK12

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
CI-1040 ROCK1

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
CI-1040 RPS6KB1

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
CI-1040 CHEK1

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
CI-1040 MAPK8

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
CI-1040 KRAS

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type colorectal cancer

Response Type sensitive

Approval Status Preclinical

PMIDs:
19018267 19372556

Sources:
JAX-CKB
CI-1040 GSK3B

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
CI-1040 LCK

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
CI-1040 MAPK14

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
CI-1040 AKT1

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
CI-1040 ERBB2

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type breast cancer

Response Type resistant

Approval Status Preclinical

PMIDs:
23948973

Sources:
JAX-CKB
CI-1040 MAPK1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD

MyCancerGenome: CI-1040
- Version: 20-Jun-2017
Alternate Names:

Drug Info:

Drug Class Kinase Inhibitors

Notes allosteric inhibitor

Publications:

DTC: CI-1040

Version: 02-September-2020

Alternate Names:

CHEMBL105442 ChEMBL Drug ID

Drug Info:

Publications:

Li Q et al., 2010, Discovery of 3-(2-aminoethyl)-5-(3-phenyl-propylidene)-thiazolidine-2,4-dione as a dual inhibitor of the Raf/MEK/ERK and the PI3K/Akt signaling pathways., Bioorg Med Chem Lett

JAX-CKB: CI-1040

Version: 27-September-2017

Alternate Names:

Drug Info:

Publications:

Delaney et al., 2002, Identification of a novel mitogen-activated protein kinase kinase activation domain recognized by the inhibitor PD 184352., Mol. Cell. Biol.

Emery et al., 2009, MEK1 mutations confer resistance to MEK and B-RAF inhibition., Proc. Natl. Acad. Sci. U.S.A.

Whittaker et al., 2010, Gatekeeper mutations mediate resistance to BRAF-targeted therapies., Sci Transl Med

TTD: CI-1040
- Version: 2020.06.01
Alternate Names:

D0B9BU TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL105442
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL105442
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:

Indication/Tumor Type	melanoma
Response Type	resistant
Approval Status	Preclinical - Cell culture

Evidence Type	Actionable
Approval Status	Preclinical - Cell culture
Response Type	sensitive

Mechanism of Interaction	Dual specificity mitogen-activated protein kinase kinase 2 inhibitor
Direct Interaction	yes

Indication/Tumor Type	Advanced Solid Tumor
Response Type	sensitive
Approval Status	Preclinical

Indication/Tumor Type	colorectal cancer
Response Type	sensitive
Approval Status	Preclinical

Indication/Tumor Type	breast cancer
Response Type	resistant
Approval Status	Preclinical

allosteric modulator
inhibitor (inhibitory)

CI-1040 Drug Record

CI-1040 chembl:CHEMBL105442 Antineoplastic

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 20580230

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: allosteric modulator inhibitor (inhibitory)

Interaction Info: Indication/Tumor Type melanoma Response Type resistant Approval Status Preclinical - Cell culture

PMIDs: 12370306 19915144

Sources: MyCancerGenome JAX-CKB ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info: Evidence Type Actionable Approval Status Preclinical - Cell culture Response Type sensitive

PMIDs: 27821489

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type melanoma Response Type sensitive Approval Status Preclinical

PMIDs: 26267534

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Mechanism of Interaction Dual specificity mitogen-activated protein kinase kinase 2 inhibitor Direct Interaction yes

PMIDs: None found

Sources: MyCancerGenome ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type Advanced Solid Tumor Response Type sensitive Approval Status Preclinical

PMIDs: 19018267 19915144 20538618

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info: Indication/Tumor Type colorectal cancer Response Type sensitive Approval Status Preclinical

PMIDs: 19018267 19372556

Sources: JAX-CKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
20580230

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

allosteric modulator

inhibitor (inhibitory)

Interaction Info:

Indication/Tumor Type melanoma

Response Type resistant

Approval Status Preclinical - Cell culture

PMIDs:
12370306 19915144

Sources:
MyCancerGenome JAX-CKB ChemblInteractions

Interaction Types & Directionality:

n/a

Interaction Info:

Evidence Type Actionable

Approval Status Preclinical - Cell culture

Response Type sensitive

PMIDs:
27821489

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type melanoma

Response Type sensitive

Approval Status Preclinical

PMIDs:
26267534

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Mechanism of Interaction Dual specificity mitogen-activated protein kinase kinase 2 inhibitor

Direct Interaction yes

PMIDs:
None found

Sources:
MyCancerGenome ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type Advanced Solid Tumor

Response Type sensitive

Approval Status Preclinical

PMIDs:
19018267 19915144 20538618

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type colorectal cancer

Response Type sensitive

Approval Status Preclinical

PMIDs:
19018267 19372556

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

n/a

Interaction Info:

Indication/Tumor Type breast cancer

Response Type resistant

Approval Status Preclinical

PMIDs:
23948973

Sources:
JAX-CKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Drug Info:

Drug Class Kinase Inhibitors

Notes allosteric inhibitor

Alternate Names:

CHEMBL105442 ChEMBL Drug ID

Publications:

Li Q et al., 2010, Discovery of 3-(2-aminoethyl)-5-(3-phenyl-propylidene)-thiazolidine-2,4-dione as a dual inhibitor of the Raf/MEK/ERK and the PI3K/Akt signaling pathways., Bioorg Med Chem Lett

Alternate Names:

D0B9BU TTD Drug ID