U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

Showing 21 - 30 of 473 results

Status:
Investigational
Source:
NCT03426605: Phase 1 Interventional Completed Oncology
(2018)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

MPC-3100 is a fully synthetic, orally bioavailable, Hsp90 inhibitor developed by Myriad Pharmaceuticals, Inc for cancer treatment. MPC-3100 targets the N-terminal ATP-binding site of Hsp90 and blocks the activity of ATPase. MPC-3100 shows a broad spectrum anti-proliferative activity against various cancer cell lines, such as HCT-116, NCI-N87 and DU-145. MPC-3100 also inhibits tumor growth in the NCI-N87 gastric cancer xenograft mode. Moreover, pharmacokinetics studies show that MPC-3100 displays a superior oral pharmacokinetics profile, good overall exposure and a reasonable hepatic clearance rate. Phase I clinical studies demonstrate MPC-3100 is safe and tolerated when administered at doses below 600 mg per day
Status:
Investigational
Source:
NCT01985191: Phase 1 Interventional Completed Neoplasm Malignant
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

SAR-405838 is an inhibitor of the interaction between the oncoprotein murine double minute 2 (MDM2) and p53. SAR-405838 was investigated in phase I clinical trials in patients with locally advanced/metastatic solid tumor with wild-type TP53 or with TP53 mutation prevalence below 40%. SAR-405838 had an acceptable safety profile with limited activity in patients with advanced solid tumors.
Status:
Investigational
Source:
NCT01779427: Not Applicable Interventional Withdrawn Traumatic Brain Injury (TBI)
(2013)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

p53 is a critical tumor suppressor and is the most frequently inactivated gene in human cancer. Inhibition of the interaction of p53 with its negative regulator MDM2 represents a promising clinical strategy to treat p53 wild-type tumors. AMG 232 is a potential best-in-class inhibitor of the MDM2-p53 interaction and is currently in clinical trials. Based on X-ray cocrystal structures a model of AMG 232 bound to MDM2 was developed. The model shows that the m-chlorophenyl, the p-chlorophenyl, and C-linked isopropyl fragments of AMG 232 bind to the Leu 26(p53), Trp 23(p53), and Phe 19(p53) pockets of MDM2, respectively. The carboxylic acid forms a salt bridge with His 96 and the isopropyl sulfone forms a novel interaction with the glycine shelf region of MDM2. AMG 232 in phase II in combination with trametinib and dabrafenib in subjects with metastatic melanoma; in phase I for the treatment of solid tumors, multiple myeloma and Acute Myeloid Leukemia.
Status:
Investigational
Source:
JAN:1-(4-METHYLPHENYL) ETHYL NICOTINATE [JAN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

3-Pyridinecarboxylic acid, 1-(4-methylphenyl)ethyl ester is an choleretic agent.
Status:
Investigational
Source:
NCT01693159: Not Applicable Interventional Unknown status Pain
(2011)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT01121614: Not Applicable Interventional Completed Surgery
(2008)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Cinidon-ethyl (BAS 615H) is a herbicide of isoindoldione class which selectively controls a wide spectrum of broadleaf weeds in cereals. Cinidon‐ethyl strongly inhibited protoporphyrinogen oxidase (Protox) activity in vitro, with I50 values of approximately 1 nM for the enzyme isolated from the weed species and from wheat. Cinidon-ethyl was approved in the EU in the early 2010s, but authorization was revoked due to lack of interest from the applicant.
Status:
Investigational
Source:
NCT03184545: Phase 3 Interventional Recruiting Patellofemoral Pain Syndrome
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
Cancer. Aug 1993;72(4):1184-91.: Phase 2 Human clinical trial Completed Neoplasm Recurrence, Local/mortality
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
INN:bentamapimod [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Bentamapimod (AS602801) a newly developed, orally-active, ATP competitive inhibitor of JNK, which is in phase IIa clinical trials for the treatment of endometriosis. Bentamapimod showed selective cytotoxic activity against serum-cultured cancer cells and cancer stem cells in vitro. It blocks T-cell proliferation and induces apoptosis. Bentamapimod was discovered by Merck Serono. Then PregLem (a member of the Richter Group) acquired worldwide rights in 2010.