adenosine antagonist 1

Adenosine antagonist-1 acts as an adenosine A3 receptor (AA3R) antagonist.

Adenosine receptor A1 antagonist 5 acts as an adenosine antagonist, is an oxypurine, acts as an insecticide and pest control agent, and has an inhibitory effect on elevated blood pressure.

Adenosine receptor antagonist 1 is a highly selective A2aR adenosine receptor antagonist with an IC50 value of 0.29 nM and shows a 14-fold greater selectivity for A2aR over A2bR.

A2B receptor antagonist 1 (EXAMPLE 9B) is a potent A2B adenosine receptor antagonist.

CGRP antagonist 1 is a potent CGRP receptor antagonist with Ki values of 35 nM and IC50 values of 57 nM, respectively.CGRP antagonist 1 can be used for the study of cardiovascular and neurovascular diseases.

Y1 receptor antagonist 1 (H 409-22 isomer) is the active isomer of H-409/22, a neuropeptide Y (NPY) Y1 receptor antagonist that dose-dependently antagonizes the vascular response to exogenous and endogenous NPY in pigs. lagodeoxycholic acid (H 409-22 isomer) is the active isomer of H-409/22, an antagonist of neuropeptide Y (NPY) Y1 receptor.

Hepcidin antagonist-1 is an iron-modulating antagonist.Hepcidin antagonist-1 can be used to study metabolic disorders such as iron-deficiency diseases and anemia.

5-HT6 7 antagonist 1 is a dual 5-HT6 7 2A and D2 receptor antagonist used in the study of dementia and Alzheimer's disease.

EP1-antagonist-1 (EP1 antagonist 1) is an EP1 antagonist (pKi: 7.54; pIC50: 8.5).

LPA1 receptor antagonist 1(LPA1 R antagonist 1) is a selective and potent lysophosphatidic acid (LPA1) receptor antagonist (IC50 : 25 nM) for the study of idiopathic pulmonary fibrosis.

ORL1 antagonist 1 is an o antagonist of pioid receptor-like 1 (ORL1) (IC50 of 61 nM).

AR antagonist 1 is a potent antagonist of the androgen receptor. It binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266.

CRTh2 antagonist 1 is a CRTh2 antagonist [IC50: 89 nM].

5-HT2 antagonist 1 is a potent 5-HT2 receptor antagonist with weak α1 adrenoceptor blocking activity.

A2A receptor antagonist 1 (CPI-444 analog) is an inhibitor of the adenosine A2A receptor and A1 receptor with Ki values of 4 nM and 264 nM, respectively.

5-HT2A antagonist 1 is a 5-HT2A receptor blocker that may be useful in treating gastrointestinal and circulatory disorders.

Dopamine D2 Receptor Antagonist-1 functions as a negative allosteric modulator (NAM) of the dopamine D2 receptor (D2R), demonstrating sub-millimolar affinity.

Androgen receptor antagonist 1, an orally available full androgen receptor antagonist (IC50: 59 nM), is utilized in the synthesis of PROTAC AR degraders, achieving 24% and 47% AR protein degradation in LNCaP cells at concentrations of 1 μM and 10 μM, respectively.

5-HT4 antagonist 1 is an antagonist of 5-HT4 (pKi = 9.6).

Sigma-1 receptor antagonist 2 is a more potent and selective antagonist of the sigma-1 receptor (σ1 R, Ki = 3.88 nM) compared to the sigma-2 receptor (Ki = 1288 nM).

H3 receptor antagonist 1 is used in the study of neurological diseases, histamine H3 receptor antagonist.

ERRα antagonist-1 (ERR+/- antagonist-1) is a high-affinity, selective antagonist of the estrogen-related receptor α (ERRα). It effectively prevents the interaction of ERRα with both Proliferator-activated Receptor γ Coactivator-1α (PGC-1α) and PGC-1β, displaying IC50 values of 170 nM and 180 nM, respectively. Notably, ERRα antagonist-1 does not interfere with the interactions involving ERRβ or ERRγ and the PGC-1α and PGC-1β coactivators. Furthermore, it does not affect the interaction between either ERα or ERβ and PGC-1α or SRC-1.

(E)-GABAB receptor antagonist 1 is a trans-GABAB receptor antagonist that decreases GABA-induced IP3 (inositol trisphosphate) production with an IC50 of 37.9 μM. It is a selective and negative allosteric modulator of GABAB (γ-Aminobutyric acid) receptors.

N-(6-chloro-5-(2-Methoxyphenoxy)-2-(pyridin-4-yl)pyriMidin-4-yl)-5-Met inhibits endothelin binding to membranes from CHO cells carrying human ETA receptor and human ETB receptor with IC50 of 268nM and 1810nM, respectively.

Adenosine receptor antagonist 4 is an adenosine receptor antagonist.

Sigma-1 receptor antagonist 3 is a potent and selective antagonist of Sigma-1 (σ1) receptor(Ki : 1.14 nM), has the potential for the neuropathic pain.

CCR3 antagonist 1 is a potent CCR3 antagonist used in researching inflammatory and immunologic diseases.

hGPR91 antagonist 1 is a potent and selective hGPR91 antagonist (IC50: 7 μM).

GluR6 antagonist-1 inhibits the pY binding site of tyrosine kinase p56lck SH2 domain.

H4 Receptor antagonist 1 is a potent and selective histamine H4 receptor inverse agonist with an IC50 of 19 nM.

NMDAR antagonist 1 is an orally active, NR2B-selective NMDAR antagonist.

σ1 Receptor antagonist-1 is a selective σ1 receptor antagonist.

TMBIM6 antagonist-1 (BAX-inhibitor-1) is a bax inhibitor

Adenosine receptor inhibitor 1 is a highly potent and selective antagonist of adenosine receptor (AR), exhibiting exceptional affinity for A1 AR, A2A AR, A2B AR, and A3 AR, with respective Ki values of >1000, 68.5, >1000, >1000 nM. This compound demonstrates notable antinociceptive, anti-inflammatory, and peripheral analgesic properties, holding great promise for investigating cancer and neurodegenerative diseases [1].

A1/A3 AR antagonist 1 (Compound 10) is a potent, dual adenosine 1 (A1) and adenosine 3 (A3) receptor antagonist that acts on human A1 (Ki: 37.6 nM), human A3 (Ki: 25.4 nM) and rat A1 (Ki: 1.47 nM). 1 Can be used to study renal failure, inflammatory lung disease and Alzheimer's disease.

Adenosine receptor antagonist 3 has the potential for cancer disease research which is a potent adenosine receptor antagonist [1].

A2AAR antagonist 1 (compound 21a) is a potent A2AAR (adenosine A2A receptor) antagonist with high ligand efficiency and a Ki value of 20 nM. It is applicable in neurodegenerative disease research [1].

A1AR antagonist 1 (compound 18g) is a potent A1 adenosine receptor (AR) antagonist with Ki values of 2.08, 6.91, and 31.2 nM for hA1, hA2A, and hA2B, respectively [1].

A2AR-antagonist-1 (compound 38), an orally active adenosine A2A receptor antagonist with an IC50 value of 29 nM, demonstrates anti-tumor properties and stability in mouse liver microsomes (t1/2 = 86.1 min). Additionally, it activates T cells by inhibiting immunosuppressive molecules (LAG-3 and TIM-3) and promoting expression of effector molecules (GZMB, IFNG, and IL-2) [1].

Compound 23, designated as A2A/A3 AR antagonist-1, is a dual fluorescent ligand targeting A2A and A3 adenosine receptors (AR), exhibiting dissociation constants (Ki) of 90 nM for hA2A AR and 31.8 nM for hA3 AR, respectively [1].

Adenosine receptor antagonist 2 is an orally active A2a (IC50: 1 nM) and A2b (IC50: 3 nM) adenosine receptor antagonist with antitumor properties.

CDK9 Antagonist-1 (compounds 11c) is a potent and selective CDK9 degrader based on PROTAC, with an IC50 of 17 μM in MCF-7 cell lines. Natural product Wogonin binds ubiquitin E3 ligase cereblon (CRBN) via a linker to form PROTAC[1]. CDK9|17 μM (IC50, MCF-7 cells) [1]. Bian J , et al. Discovery of Wogonin-based PROTACs against CDK9 and capable of achieving antitumor activity. Bioorg Chem. 2018 Dec;81:373-381.

TRPA1 Antagonist 1 is an antagonist of TRPA1(IC50: 8 nM) and is a methylene phosphate prodrug which converts to its active parent drug.

Substance P Receptor Antagonist 1 has potential applications in treating gastrointestinal disorders, inflammatory diseases, respiratory conditions, and central nervous system disorders.

CCR5 antagonist 1, derived from WO 2004054974 A2, is a CCR5 antagonist that inhibits HIV replication.

XIAP cIAP1 antagonist-1 is a potent, orally active XIAP cIAP1 antagonist with an EC50 of 5.1 nM for XIAP and 0.32 nM for cIAP1, and dose-dependently inhibits tumor growth in vivo.

BLT2 antagonist-1 (compound 15b) is a selective inhibitor of the BLT2 receptor, impeding the chemotaxis of CHO-BLT2 cells at an IC50 of 224 nM without affecting CHO-BLT1 cell chemotaxis. It blocks the interaction between LTB4 and the BLT2 receptor with a K_i of 132 nM and may serve as a research tool for inflammatory airway diseases, including asthma and chronic obstructive pulmonary disease [1].

GABA receptor Antagonist 1 (compound 7w) effectively inhibits the Px RDL1 GABAR at an IC50 of 7.08 nmol L and demonstrates insecticidal efficacy against P. xylostella, S. frugiperda, S. exigua, and S. litura with respective LC50 values of 0.09, 0.84, 0.87, and 0.68 mg L. This compound also exhibits moderate toxicity to honeybees (48 h, ID50 = 2.22 μg adult) and low toxicity to zebrafish (LC50: 42.4 mg L) [1].

DB21, Galectin-1 Antagonist, is a peptidomimetic conjugated with dibenzofuran, serving as an allosteric inhibitor of galectin-1 (GAL1) interactions with glycans on cell surfaces. This compound enhances the inhibition of angiogenesis and tumor growth in melanoma, lung adenocarcinoma, and ovarian cancer models [1].

CMKLR1 antagonist 1 (compound S-26d) is a potent, orally active antagonist of the chemokine-like receptor 1 (CMKLR1) with a pIC50 of 7.44 in hCMKLR1-transfected CHO cells, applicable in the research of psoriasis and metabolic diseases [1].