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adenylyl cyclase inhibitor
SQ22536 is an inhibitor of adenylyl cyclase with an IC50 of 1.4 uM. It can inhibit PGE1-stimulated increases in cAMP levels in intact human platelets.- Adrian Hilman, .et al. , FASEB J, 2026, Mar 31;40(6):e71696 PMID: 41847922
- Ke Qian, .et al. , EBioMedicine, 2023, Dec:98:104863 PMID: 37950995
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DAT and SLC6A2 inhibitor
GBR-12935 is a piperazine derivative which is a potent and selective dopamine reuptake inhibitor.- Alexander D H Kingdon, .et al. , J Antibiot (Tokyo), 2025, Jan;78(1):54-63 PMID: 39402358
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dopamine re-uptake inhibitor
Vanoxerine (GBR-12909) is a piperazine derivative which is a potent and selective DRI.- Alexander D H Kingdon, .et al. , J Antibiot (Tokyo), 2025, Jan;78(1):54-63 PMID: 39402358
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human A3 adenosine receptor antagonist /Aurora inhibitor
Reversine is a potent human A3 adenosine receptor antagonist with Ki of 0.66 μM, and a pan-aurora A/B/C kinase inhibitor with IC50 of 12 nM/13 nM/20 nM, respectively. Also used for stem cell dedifferentiation.- Amy H. Ide, .et al. , Mol Biol Cell, 2023, Jun 1;34(7):ar76 PMID: 37126397
- Hazheen K, .et al. , J Biol Chem, 2020, August 20 PMID: 32820050
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DPP-4 Inhibitor
Linagliptin is a DPP-4 inhibitor, an enzyme that degrades the incretin hormones glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP).- Fen Zhuge, .et al. , Exp Neurol, 2024, Mar:373:114689 PMID: 38199510
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Androgen Receptor inhibitor
ARN-509 is an androgen receptor antagonist with potential antineoplastic activity. ARN-509 binds to AR in target tissues thereby preventing androgen-induced receptor activation and facilitating the formation of inactive complexes that cannot be translocated to the nucleus. This prevents binding to and transcription of AR-responsive genes.- Frédérique Mittler, .et al. , Front Oncol, 2017, 7: 293 PMID: 29322028
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peptide Oxytocin Receptor Inhibitor
Atosiban is a peptide Oxytocin Receptor Inhibitor.- G Perez-Hernandez, .et al. , J Dairy Sci, 2023, Dec;106(12):9855-9867 PMID: 37641323
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Adenosine kinase inhibitor
5-Iodotubercidin is a potent adenosine kinase inhibitor with IC50 of 26 nM.- Jing-Yu Lin, .et al. , Cell Discov, 2020, 6: 20 PMID: 32284878
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CXCL8/CXCR1/2 Inhibitor
Reparixin is a potent inhibitor of both CXCL8 receptors CXCR1/2, it inhibits weakly CXCR2-mediated cell migration (IC50=100 nM), whereas it strongly blocks CXCR1-mediated chemotaxis (IC50=1 nM).- Naour AL, .et al. , J Mol Cell Biol, 2019, Sep 3 PMID: 31504643
- Wigenstam E, .et al. , Toxicology, 2015, Feb 3;328:40-7 PMID: 25497111
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Serotonin reuptake inhibitor
Escitalopram oxalate ((S)-(+)Citalopram oxalate) is a selective serotonin reuptake inhibitor (SSRI) with Ki of 0.89 nM.- Reilly Taylor, .et al. , Front. Biosci. (Elite Ed), 2026, 18(1): 44075 PMID: 41914162
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S1P inhibitor
PF429242 dihydrochloride is a reversible and competitive S1P inhibitor with an IC50 of 175 nM.- Shiying Xie, .et al. , FEBS J, 2024, Apr;291(7):1575-1592 PMID: 38243371
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GluR inhibitor
(-)-Huperzine A is a naturally occurring sesquiterpene alkaloid compound found in the firmoss Huperzia serrata.- Takuya Ohba, .et al. , PharmaNutrition, 2020, 13:100203
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Smoothened inhibitor
BMS-833923 (or XL-139) is an orally bioavailable small-molecule SMO (Smoothened) inhibitor with potential antineoplastic activity.- Valérian Pasche, .et al. , Parasit Vectors, 2018, 11: 298 PMID: 29764454
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PAFR inhibitor/H1 receptor inhibitor
Rupatadine is an inhibitor of PAFR and histamine (H1) receptor with Ki of 550 and 102 nM, respectively. -
CXCR4 Inhibitor
MSX-122 is an orally bioavailable inhibitor of CXCR4 (IC50 = ~10 nM) with potential antineoplastic and antiviral activities. CXCR4 inhibitor MSX-122 binds to the chemokine receptor CXCR4, preventing the binding of stromal derived factor-1 (SDF-1) to the CXCR4 receptor and receptor activation, which may result in decreased tumor cell proliferation and migration. -
SphK2 inhibitor
ABC294640 is an orally available, aryladamantane compound and selective inhibitor of sphingosine kinase-2 (SK2) with potential antineoplastic activity. -
Adenosine receptor inhibitor
N-[(4-Aminophenyl)methyl]adenosine is a adenosine receptor inhibitor, with Ki of 29 nM for Rat ecto-5??-Nucleotidase. IC50 value: 29.0 ± 1.7 nM (Ki) Target: Adenosine Receptor -
Smoothened Inhibitor
LDE225 is an orally bioavailable small-molecule Smoothened (Smo) antagonist with potential antineoplastic activity. -
Smoothened Inhibitor
PF-5274857 is a novel Smo antagonist that specifically binds to Smo with a K(i) of 4.6 ?? 1.1 nmol/L and completely blocks the transcriptional activity of the downstream gene Gli1 with an IC(50) of 2.7 ?? 1.4 nmol/L in cells. -
S1PR1/S1PR5 inhibitor
BAF312 is a next-generation potent sphingosine 1-phosphate (S1P) receptor agonist, selective for S1P1 and S1P5. -
dopamine uptake inhibitor
GBR 12783 dihydrochloride is a very potent and selective inhibitor of dopamine uptake (IC50 for inhibition of [3H]-dopamine uptake in rat striatal synaptosomes is 1.8 nM). -
norepinephrine (NE) transporter inhibitor
Atomoxetine hydrochloride is a competitive and specific inhibitor of SLC6A2 while demonstrating weak ST and DAT inhibition as studied in synaptosomes of rat hypothalamus. -
serotonin uptake inhibitor
Norfluoxetine is an active metabolite of the antidepressant fluoxetine that inhibits serotonin uptake with a pKi value of 7.35.1 The S-enantiomer of norfluoxetine has 20-times higher serotonin reuptake blocking potency than the R-enantiomer (pKis = 7.86 versus 6.51, respectively). -
human 5'-methylthioadenosine phosphorylase inhibitor
MT-DADMe-ImmA is an inhibitor of human 5'-methylthioadenosine phosphorylase (MTAP) with a Ki of 90 pM. -
dopamine β-hydroxylase (DBH) inhibitor
Zamicastat (BIA 5-1058) is a dopamine β-hydroxylase (DBH) inhibitor that could cross the blood-brain barrier (BBB) and cause central as well as peripheral effects. -
norepinephrine reuptake inhibitor
Edivoxetine HCl is a drug which acts as a selective norepinephrine reuptake inhibitor -
Smoothened inhibitor
PF-04449913 is a potent and orally bioavailable inhibitor of smoothened. -
angiotensin receptor-neprilysin inhibitor
LCZ696 is an orally bioavailable, dual-acting angiotensin receptor-neprilysin inhibitor (ARNi) for hypertension and heart failure. -
serotonin/NE reuptake inhibitor
Levomilnacipran HCl is a selective serotonin and norepinephrine reuptake inhibitor. -
alpha-adrenergic receptor agonist / MAO inhibitor
Amitraz, also known as Mitaban and Taktic, is an alpha-adrenergic receptor agonist and MAO inhibitor used as an insecticide in prevention of flea and tick infections. It prevents prostaglandin synthesis and may inhibit beta-cell insulin release. -
D2DR and D4DR inhibitor
Loxapine Succinate is a D2DR and D4DR inhibitor and serotonergic receptor antagonist. Loxapine succinate is an antipsychotic agent used in schizophrenia. -
Prostaglandin Receptor inhibitor
Benorilate, also known as Win-11450, is an ester of aspirin and paracetamol with analgesic, antipyretic, and anti-inflammatory activity used in the treatment of rheumatoid diseases. Benorilate has less severe side effects than aspirin. -
Prostaglandin Receptor inhibitor
Dinoprost Tromethamine, also known as Dinoprost Trometamol, is a naturally occurring prostaglandin used in medicine to induce labor and as an abortifacient. -
serotonin uptake inhibitor
Paroxetine Mesylate is a serotonin uptake inhibitor that is effective in the treatment of depression. -
5-HT2 receptors inhibitor
Nefazodone HCl is an inhibitor of 5-HT2 receptors, SERT, NET, and hERG K+ channels used to treat mood disorders. It decreases immobility time in the forced swim test. -
D2DR inhibitor
Promazine Hydrochloride is a phenothiazine compound and D2DR inhibitor. Promazine Hydrochloride has been employed in studies investigating dopamine-stimulated glycosylation of brain proteins in vitro. It has actions similar to chlorpromazine but with less antipsychotic activity. -
MAO inhibitor
Molindone HCl is a D2 dopamine receptor antagonist. It also acts as a MAO inhibitor.

