DC23371 |
NI-42
Featured
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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. |
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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. |
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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. |
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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). |
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DC20689 |
ASB 14780 |
A potent, selective and orally active cytosolic phospholipase A2α (cPLA2α) inhibitor with IC50 of 20 nM. |
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DC21689 |
SR 142948A
Featured
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A potent, selective and orally active neurotensin receptor antagonist with IC50 of 1.19 nM. |
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DC23621 |
YM543 |
A potent, selective and orally active SGLT2 inhibitor with IC50 of 8.9 nM, 280-fold selectivity over SGLT1. |
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DC21842 |
Darexaban |
A potent, selective and orally available factor Xa (FXa) inhibitor with IC50 of 54.6 nM. |
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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. |
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DC20768 |
Tonapofylline |
A potent, selective and orally bioavailable adenosine A1 (A1A) receptor antagonist with Ki of 7 nM. |
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DC22682 |
INCB9471 |
A potent, selective and orally bioavailable CCR5 antagonist IC50 of 6.5 nM, Kd of 3.1 nM in human PBMCs. |
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DC23643 |
JNJ 54166060 |
A potent, selective and orally bioavailable P2X7 receptor with IC50 of 4 nM and 115 nM for hP2X7 and rP2X7, respectively. |
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DC21600 |
S1P Lyase inhibitor 31 |
A potent, selective and orally bioavailable S1P lyase (S1PL) inhibitor with enzyme IC50 of 44 nM, cell IC50 of 110 nM. |
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DC23207 |
JNJ-17203212
Featured
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A potent, selective and orally bioavailable TRPV1 receptor antagonist with IC50 of 65 nM and 102 nM for hTRPV1 and rTRPV1, respectively. |
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DC21464 |
Eribaxaban |
A potent, selective and orally efficacious factor Xa (FXa) inhibitor with IC50 of 0.32 nM. |
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DC25047 |
Calphostin C |
A potent, selective and photo-dependent inhibitor of PKC with IC50 of 50 nM. |
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DC20602 |
5F 203
Featured
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A potent, selective antitumour agent through activation the aryl hydrocarbon receptor (AhR) pathway. |
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DC21576 |
RO-5508887 |
A potent, selective BACE inhibitor with IC50 of 30 nM for BACE1, equally potent against BACE2 (IC50=40 nM) but >1,000-fold selectivity over cathepsin D, cathepsin E, pepsin and renin. |
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DC21103 |
GW405833 hydrochloride |
A potent, selective cannabinoid receptor CB2 agonist with Ki of 3.6 nM, 1200-fold selectivity over CB1. |
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DC20658 |
AM1241
Featured
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A potent, selective cannabinoid receptor CB2 agonist with Ki of 7.1 nM, >80-fold selectivity over CB1 receptors in radioligand binding assay. |
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DC21376 |
NESS-0327 |
A potent, selective CB1 cannabinoid receptor antagonist with Ki of 350 fM, >60,000-fold selective for the CB1 receptor versus CB2 receptor (Ki=21 nM). |
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DC23357 |
CBP bromodomain inhibitor |
a potent, selective CBP bromodomain inhibitor with IC50 of 69 nM, displays exquisite selectivity over BRD4(1) (IC50=18 uM) and the broader bromodomain family.. |
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DC22697 |
PF-04756956 |
A potent, selective CCK1 receptor agonist with EC50 of 0.47 nM. |
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DC21393 |
nNOS-IN-25 |
A potent, selective cell permeable neuronal nitric oxide synthase (nNOS) inhibitor with Ki of 30 nM. |
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DC20633 |
ACG-548B |
A potent, selective choline kinase α (ChoKα) inhibitor with IC50 of 0.12 uM, >400-fold selectivity over ChoKβ. |
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DC20632 |
ACG-416B |
A potent, selective choline kinase α (ChoKα) inhibitor with IC50 of 0.13 uM, >385-fold selectivity over ChoKβ. |
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DC21741 |
RSM-932A |
A potent, selective choline kinase α (ChoKα) inhibitor with IC50 of 1.0 uM, 33-fold selectivity over ChoKβ. |
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DC22917 |
SCH 79797 dihydrochloride
Featured
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A potent, selective competitive and nonpeptide PAR-1 antagonist with IC50 of 70 nM. |
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DC20580 |
Vitacoxib |
A potent, selective COX-2 inhibitor with IC50 of 0.34 ug/mL, >50-fold selectivity over COX-1 (IC50=19.4 ug/mL). |
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DC22418 |
CCX-771 |
A potent, selective CXCR7 antagonist with IC50 of 4.1 nM. |
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