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Originator

Chiron

7

Pfizer

420

Eli Lilly

237

Merck

216

GlaxoSmithKline

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Primary Target

Glycogen synthase kinase-3 alpha

4

Glycogen synthase kinase-3 beta

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Serine/threonine-protein kinase Chk1

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Unknown

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Type 2 diabetes mellitus

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Unknown

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Breast cancer

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Showing 1 - 7 of 7 results

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BIPENAMOL

49DCB7156W

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Status:

Investigational

Class (Stereo):

CHEMICAL (ACHIRAL)

Conditions:

Bipenamol is a benzenemethanol derivative used to prepare novel semicarbazide-derived inhibitors of human dipeptidyl peptidase I.

LADUVIGLUSIB

234CMT4GK4

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Status:

Investigational

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Glycogen synthase kinase-3 alpha

Glycogen synthase kinase-3 beta

Conditions:

Type 2 diabetes mellitus

CHIR 99021 is a selective, pyridimidine-based, glycogen synthase kinase 3 inhibitor that is effective at low nanomolar concentrations in enzyme assays and submicromolar concentrations in isolated cells and tissues. Chiron was developing CHIR 99021 fo...

r potential use in the treatment of type 2 diabetes mellitus. CHIR 99021 promoted insulin-mediated glucose uptake and increased glucose disposal in rodent models of diabetes. However, there has been no recent development reported.

CHIR-124

5K64W8EU3E

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Status:

Other

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Serine/threonine-protein kinase Chk1

Conditions:

CHIR-124 is a quinolone-based small molecule that is structurally unrelated to other known inhibitors of Chk1. CHIR-124 potently and selectively inhibits Chk1 in vitro. CHIR-124 interacts synergistically with topoisomerase poisons (e.g., camptothecin...

or SN-38) in causing growth inhibition in several p53-mutant solid tumor cell lines. CHIR-124 abrogates the SN-38-induced S and G(2)-M checkpoints and potentiates apoptosis in MDA-MD-435 breast cancer cells. CHIR-124 treatment can restore the level of cdc25A protein, which is normally targeted by Chk1 for degradation following DNA damage, indicating that Chk1 signaling is suppressed in the presence of CHIR-124. In an orthotopic breast cancer xenograft model, CHIR-124 potentiates the growth inhibitory effects of irinotecan by abrogating the G(2)-M checkpoint and increasing tumor apoptosis. The combination of gemcitabine and CHIR-124 in the multicellular tumor spheroid model enhanced the sensitivity to the gemcitabine antiproliferative effect in correlation with an increase in DNA damage and apoptosis. CHK1 inhibition by Chir-124 sensitizes HCT116 cancer cells to radiation.

LADUVIGLUSIB DIHYDROCHLORIDE

X6BE5J2G31

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Status:

Investigational

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Glycogen synthase kinase-3 alpha

Glycogen synthase kinase-3 beta

Conditions:

Type 2 diabetes mellitus

CHIR 99021 is a selective, pyridimidine-based, glycogen synthase kinase 3 inhibitor that is effective at low nanomolar concentrations in enzyme assays and submicromolar concentrations in isolated cells and tissues. Chiron was developing CHIR 99021 fo...

r potential use in the treatment of type 2 diabetes mellitus. CHIR 99021 promoted insulin-mediated glucose uptake and increased glucose disposal in rodent models of diabetes. However, there has been no recent development reported.

LADUVIGLUSIB TRIHYDROCHLORIDE

LMF6N91874

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Status:

Investigational

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Glycogen synthase kinase-3 alpha

Glycogen synthase kinase-3 beta

Conditions:

Type 2 diabetes mellitus

CHIR 99021 is a selective, pyridimidine-based, glycogen synthase kinase 3 inhibitor that is effective at low nanomolar concentrations in enzyme assays and submicromolar concentrations in isolated cells and tissues. Chiron was developing CHIR 99021 fo...

r potential use in the treatment of type 2 diabetes mellitus. CHIR 99021 promoted insulin-mediated glucose uptake and increased glucose disposal in rodent models of diabetes. However, there has been no recent development reported.

LADUVIGLUSIB HYDROCHLORIDE

5AW8G37ZX5

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Status:

Investigational

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Glycogen synthase kinase-3 alpha

Glycogen synthase kinase-3 beta

Conditions:

Type 2 diabetes mellitus

CHIR 99021 is a selective, pyridimidine-based, glycogen synthase kinase 3 inhibitor that is effective at low nanomolar concentrations in enzyme assays and submicromolar concentrations in isolated cells and tissues. Chiron was developing CHIR 99021 fo...

r potential use in the treatment of type 2 diabetes mellitus. CHIR 99021 promoted insulin-mediated glucose uptake and increased glucose disposal in rodent models of diabetes. However, there has been no recent development reported.

BIPENAMOL HYDROCHLORIDE

65FL7UEP0F

Export Data
Search for Structure

Status:

Investigational

Class (Stereo):

CHEMICAL (ACHIRAL)

Conditions:

Bipenamol is a benzenemethanol derivative used to prepare novel semicarbazide-derived inhibitors of human dipeptidyl peptidase I.

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