| DC8540 |
DM-1(Mertansine)
Featured
|
A cytotoxic agent used in antibody-drug conjugates |
|
| DC22603 |
Dexrazoxane
Featured
|
A derivative of EDTA that chelates iron and reduces the number of metal ions complexed with anthracycline and, consequently, decrease the formation of superoxide radicals. |
|
| DC23228 |
(R)-Baclofen hydrochloride
Featured
|
A derivative of the neurotransmitter GABA that acts as a GABAB receptor agonist. |
|
| DC24088 |
Mutated EGFR-IN-1(Osimertinib analog)
Featured
|
A des acryl analogue of AZD9291 that is a useful intermediate for the inhibitors design for mutated EGFR, such as L858R EGFR, Exonl9 deletion activating mutant and T790M resistance mutant.. |
|
| DC22503 |
Val-Cit-PAB-MMAE
Featured
|
A drug-linker conjugate for Antibody-drug conjugates (ADCs) by using the anti-mitotic agent, monomethyl auristatin E (MMAE), linked via the cleavable peptide Val-Cit-PAB.. |
|
| DC20391 |
Gingerenone A
Featured
|
Gingerenone A is a Nrf2-Gpx4 activator with anti-breast-cancer properties. Gingerenone A results a delayed G2/M in cancer cells, following oxidative stress and senescence responses. Gingerenone A also alleviates ferroptosis in secondary liver injury (SLI) in dextran sodium sulfate (DSS)-induced colitis mice. Gingerenone A can be isolated from Zingiber officinale. |
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|
| DC24104 |
Almorexant
Featured
|
Almorexant(ACT078573) is a potent and competitive dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM for OX1 and OX2, respectively.IC50 value: 1.3/0.7 nM(OX1/OX2 receptor) [1] [2]Target: Dual OX!/OX2 receptorin vitro: [(3)H]Almorexant bound to a single saturable site on hOX(1) and hOX(2) with high affinity (K(d) of 1.3 and 0.17 nM, respectively. In Schild analyses using the [(3)H]inositol phosphates assay, almorexant acted as a competitive antagonist at hOX(1) and as a noncompetitive-like antagonist at hOX(2). In binding kinetic analyses, [(3)H]almorexant had fast association and dissociation rates at hOX(1), whereas it had a fast association rate and a remarkably slow dissociation rate at hOX(2) [1]. in vivo: During the 12-h dark period after dosing, ALM(Almorexant) exacerbated cataplexy in TG mice and increased nonrapid eye movement sleep with heightened sleep/wake fragmentation in both genotypes. ALM showed greater hypnotic potency in WT mice than in TG mice. The 100 mg/kg dose conferred maximal promotion of cataplexy in TG mice and maximal promotion of REM sleep in WT mice. In TG mice, ALM (30 mg/ kg) paradoxically induced a transient increase in active wakefulness [3]. Almorexant 200 mg showed significantly less 'Drug Liking' than both zolpidem doses (p < 0.01), and almorexant 400 mg had smaller effects than zolpidem 20 mg (p < 0.05), while almorexant 1,000 mg was not different from either zolpidem dose [4]. |
|
| DC22515 |
Trans-ACPD
Featured
|
trans-ACPD is a selective agonist for metabotropic glutamate receptors, acting at both group I and group II mGlu receptors. |
|
| DC20738 |
Livoletide
Featured
|
A first-in-class analogue of unacylated ghrelin, and unacylated ghrelin receptor agonist. |
|
| DC24178 |
Moxifloxacin
Featured
|
A fourth-generation synthetic fluoroquinolone, broad-spectrum antibacterial agent that is active against both Gram-positive and Gram-negative bacteria. |
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| DC22490 |
3-Bromopyruvic acid
Featured
|
A glycolytic inhibitor that inhibits hexokinase II activity, suppresses ATP production, and induces endoplasmic reticulum (ER) stress. |
|
| DC22527 |
Cyclic somatostatin
Featured
|
A growth hormone-release inhibiting factor used in the treatment of severe, acute hemorrhages of gastroduodenal ulcers. |
|
| DC22347 |
Penciclovir
Featured
|
A guanosine analogue antiviral agent used for the treatment of various herpesvirus (HSV) infections. |
|
| DC22635 |
SPDP
Featured
|
SPDP (SPDP Crosslinker) is a short-chain crosslinker for amine-to-sulfhydryl conjugation via NHS-ester and pyridyldithiol reactive groups that form cleavable (reducible) disulfide bonds with cysteine sulfhydryls. It is a glutathione cleavable ADC linker u |
|
| DC12012 |
PD 404182
Featured
|
PD 404182 is a high affinity inhibitor of KDO 8-P synthase (Ki = 26 nM). Also inhibits dimethylarginine dimethylaminohydrolase 1 (DDAH1). Exhibits antiangiogenic and antiviral activity in vitro. Putative antibiotic against gram-negative bacteria. |
|
| DC22429 |
4-BBPB
Featured
|
A highly potent agonist of σ1 receptor with Ki of 0.8 nM. |
|
| DC9843 |
AKR1C3 Inhibitor 5f
Featured
|
A highly potent and selective inhibitor of the type 5 17-β-hydroxysteroid dehydrogenase AKR1C3. |
|
| DC24083 |
4-IBP
Featured
|
A highly potent sigma receptor agonist with Ki of 1.7 nM and 25.2 nM for σ1 and σ2, respectively. |
|
| DC24063 |
Cediranib maleate
Featured
|
A highly potent, orally bioavailable, pan-VEGFR inibitor with IC50 of 1, 5, 3 nM for VEGFR1, 2, 3, respectively. |
|
| DC23424 |
RO 5256390
Featured
|
A highly potent, selective and orally bioavailable trace amine-associated receptor 1 (TRRA1) full agonist with EC50 of 18 nM, >500-fold selectivity over human adrenergic α2A receptor. |
|
| DC26071 |
BMS-814580
Featured
|
A highly potent, subtype-selective melanin concentrating hormone receptor 1 (MCHR1) inhibitor with Ki of 17 nM, without inhibitory activity for MCHR2 at 10 uM. |
|
| DC24089 |
KX2-391 mesylate
Featured
|
A highly selective, non-ATP competitive substrate-pocket-directed Src/pretubulin inhibitor. |
|
| DC24090 |
KX2-391 dihydrochloride
Featured
|
A highly selective, non-ATP competitive substrate-pocket-directed Src/pretubulin inhibitor. |
|
| DC22902 |
SNC-80
Featured
|
SNC80 (NIH 10815) is a potent, highly selective and non-peptide δ-opioid receptor agonist with a Ki of 1.78 nM and an IC50 of 2.73 nM. SNC80 also selectively activates μ-δ heteromer in HEK293 cells with an EC50 of 52.8 nM. SNC80 shows antinociceptive, antihyperalgesic and antidepressant‐like effects. SNC80 has the potential for multiple headache disorders treatment. |
|
| DC22453 |
Sappanone A
Featured
|
A homoisoflavanone found in Caesalpinia sappan, a potent, selective IMPDH2 inhibitor that covalently binds to Cys140 with Kd of 3.944 nM, almost 10 times lower than the Kd of binding to IMPDH1. |
|
| DC11590 |
Homo-PROTAC pVHL30 degrader 1
Featured
|
CM-11 is a homo-PROTAC, bivalent small-molecule dimerizer of the VHL E3 ubiquitin ligase to induce self-degradation. |
|
| DC24087 |
Calcipotriol monohydrate
Featured
|
A hormonally active metabolite of vitamin D that binds to vitamin D receptor (VDR). |
|
| DC23962 |
Cilobradine
Featured
|
A hyperpolarization-activated cyclic nucleotide-gated (HCN) channel. |
|
| DC11646 |
ML67-33
Featured
|
A low micromolar (EC50=9.7 uM, K2P2.1), selective activator of temperature- and mechano-sensitive K2P potassium channels. |
|
| DC24056 |
Agomelatine hydrochloride
Featured
|
A melatonin receptor agonist of MT1 (Ki=0.1nM) and MT2 (Ki=0.12nM), and a 5-HT2C (Ki=631nM) receptor antagonist. |
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