DC22698 |
CE-326597 |
A potent, selective agonist of the human and rat CCK1 receptor with Ki of 36 nM. |
|
DC20295 |
2-PCCA |
A potent, selective agonist of the orphan GPR88 receptor with EC50 of 877 nM. |
|
DC24029 |
PF-4840154 |
A potent, selective agonist of the rat (EC50=97 nM) and human (EC50=23 nM) TRPA1 channel. |
|
DC23831 |
TASP0382088 |
A potent, selective ALK5 inhibitor with IC50 of 4.8 nM, >100-fold selectivity over 95 different kinases. |
|
DC20564 |
TBBz
Featured
|
A potent, selective and ATP-competitive CK2 inhibitor with Ki of 0.5-1 uM. |
|
DC20686 |
AS602868 |
A potent, selective and ATP-competitive inhibitor of IKK2 with IC50 of 60 nM and Ki of 20 nM, also interfers directly with FLT3 kinase activation. |
|
DC22817 |
RUSKI-201 |
A potent, selective and cell active Hedgehog acyltransferase (Hhat) inhibitor with IC50 of 0.87 uM. |
|
DC11820 |
A-893 |
A potent, selective and cell active lysine methyltransferase SMYD2 inhibitor with IC50 of 2.8 nM. |
|
DC22867 |
HR22C16 |
A potent, selective and cell permeable inhibitor of mitotic kinesin Eg5 with IC50 of 0.8 uM, does not interact with other microtubule motor proteins. |
|
DC20309 |
ANTISAUVAGINE-30
Featured
|
A potent, selective and competitive corticotropin-releasing factor CRF2 receptor antagonist with Ki of 1.4 nM, 100-fold selectiivity over CRF1. |
|
DC11979 |
SB 332235 |
A potent, selective and competitive CXCR2 inhibitor that selectively inhibits CXCR2-mediated recruitment of β-arrestin-2 with pKi of 8.92. |
|
DC11755 |
L-732138
Featured
|
A potent, selective and competitive NK1 receptor antagonist with IC50 of 2.3 nM. |
|
DC22763 |
Rilapladib |
A potent, selective and oral lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor with IC50 of 0.23 nM, for the treatment of Alzheimer's disease and atherosclerosis.. |
|
DC21210 |
Rolofylline |
A potent, selective and orally active adenosine A1 receptor antagonist with Ki of 1.3 nM. |
|
DC21827 |
XE 991 dihydrochloride
Featured
|
A potent, selective and orally active blocker of voltage-gated potassium channels Kv7 (KCNQ) that blocks KCNQ1, KCNQ2 and KCNQ2+KCNQ3 with Kd of 0.78, 0.7 and 0.6 uM, respectively. |
|
DC23371 |
NI-42
Featured
|
NI-42 is a potent, selective and orally active BRPF1 bromodomain inhibitor with IC50 of 7.9 nM, with excellent selectivity over nonclass IV BRDs; weakly inhibits BRPF2 (BRD1), BRPF3, BRD9 and BRD4 (BD1) with IC50 of 48, 260, 310 and 4500 nM respectively, and no activity for ATAD2A/2B (IC50>100 uM); shows a modest (GI50=1-10 uM) and selective inhibition of proliferation of certain cancer lines, particularly those lines exhibiting monocytic lineage differentiation; a novel, structurally orthogonal chemical probe for the BRPFs suitable for cellular and in vivo studies. |
|
DC11710 |
GDC-0425 |
A potent, selective and orally active Chk1 inhibitor. |
|
DC24158 |
Rofecoxib |
A potent, selective and orally active COX-2 inhibitor with IC50 of 26 nM for inhibition of the COX-2-dependent production of PGE2 in human osteosarcoma cells. |
|
DC20810 |
Pexacerfont |
A potent, selective and orally active CRF1 receptor antagonist with IC50 of 6.1 nM, >1,000-fold selectivity over CRF-binding protein and biogenic amine receptors. |
|
DC20923 |
CP 376395 hydrochloride |
A potent, selective and orally active CRF1 receptor antagonist with Ki of 12 nM, shows no affinity for CRF2 receptor (Ki>10 uM). |
|
DC20689 |
ASB 14780 |
A potent, selective and orally active cytosolic phospholipase A2α (cPLA2α) inhibitor with IC50 of 20 nM. |
|
DC11868 |
Freselestat |
A potent, selective and orally active human neutrophil elastase (HNE) inhibitor with Ki of 12 nM. |
|
DC21689 |
SR 142948A
Featured
|
A potent, selective and orally active neurotensin receptor antagonist with IC50 of 1.19 nM. |
|
DC23621 |
YM543 |
A potent, selective and orally active SGLT2 inhibitor with IC50 of 8.9 nM, 280-fold selectivity over SGLT1. |
|
DC11514 |
Atogepant |
A potent, selective and orally available CGRP receptor antagonist for the prevention of migraine.
Migraine. |
|
DC21842 |
Darexaban |
A potent, selective and orally available factor Xa (FXa) inhibitor with IC50 of 54.6 nM. |
|
DC21718 |
T-3364366 |
A potent, selective and orally available inhibitor of delta-5 desaturase (D5D) with Ki of <2.7 nM and IC50 of 19 nM, with excellent selectivity over D6D and SCD. |
|
DC20768 |
Tonapofylline |
A potent, selective and orally bioavailable adenosine A1 (A1A) receptor antagonist with Ki of 7 nM. |
|
DC22682 |
INCB9471 |
A potent, selective and orally bioavailable CCR5 antagonist IC50 of 6.5 nM, Kd of 3.1 nM in human PBMCs. |
|
DC23643 |
JNJ 54166060 |
A potent, selective and orally bioavailable P2X7 receptor with IC50 of 4 nM and 115 nM for hP2X7 and rP2X7, respectively. |
|