|
T8719 |
SC99
|
|
Apoptosis
,
JAK
,
STAT
|
|
SC99 is a selective inhibitor of JAK2-STAT3 activation. SC99 downregulates the expression of STAT3-modulated genes.SC99 inhibits platelet activation, aggregation and displays potent anti-myeloma, anti-thrombotic activiti... |
|
T6541 |
Ibutilide Fumarate
|
Corvert Fumarate,U70226E |
Calcium Channel
,
Sodium Channel
|
|
Ibutilide Fumarate (U70226E) is the fumarate salt form of ibutilide, a class III antiarrhythmic agent. Ibutilide exerts its effect by activating a slow, inward, predominately sodium current rather than by blocking outwar... |
|
T8491 |
Vorolanib
|
CM082,X-82 |
VEGFR
,
PDGFR
|
|
Vorolanib (X-82) is an orally active VEGFR/PDGFR dual inhibitor. |
|
T3148 |
MK-571 sodium
|
L-660711 (sodium salt),L-660711 sodium salt,Verlukast sodium,L-660711,MK571,MK-571 sodium salt,Propanoic acid |
Leukotriene Receptor
,
LTR
|
|
MK-571 sodium (L-660711 sodium salt) is a selective, orally active antagonist of the CysLT1 receptor. MK-571 sodium is a multidrug resistance protein-2 (ABCC2, Mrp2) inhibitor used to demonstrate the role of Mrp2 in the ... |
|
T6152 |
PD318088
|
|
MEK
|
|
PD318088 is a non-ATP competitive allosteric MEK1/2 inhibitor, binding simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site. |
|
T24111 |
GSK3i XIII
|
GSK3 inhibitor XIII,GSK3iXIII,GSK3i-XIII |
GSK-3
|
|
GSK3i XIII (GSK3 inhibitor XIII) is a GSK-3 ATP-binding site inhibitor. |
|
TQ0186 |
Ko 143
|
|
BCRP
,
ABC
|
|
Ko 143 is a selective inhibitor of ATP-binding cassette sub-family G member 2 (ABCG2; BCRP). |
|
T15385 |
Glibornuride
|
|
Potassium Channel
|
|
Glibornuride is an ATP-sensitive K+ channels (KATP channel) blocker ( pKi: 5.75). It is an antidiabetic agent. |
|
T13547L |
AMP-PCP disodium
|
|
HSP
|
|
AMP-PCP disodium is an ATP analogue with binding affinity to the N-terminal domain of Hsp90, with a Kd value of 3.8 μM. The binding of AMP-PCP disodium contributes to the formation of an active homodimer of Hsp90. |
|
T12609 |
R-10015
|
|
LIM Kinase
,
Reverse Transcriptase
|
|
R-10015 is a highly potent and selective LIMK inhibitor that blocks LIMK by binding to the ATP-binding pocket. It inhibits human LIMK1 with an IC50 value of 38 nM. It also exerts broad-spectrum antiviral effects and may ... |
|
T10585 |
Bozitinib
|
CBT-101,PLB-1001 |
c-Met/HGFR
|
|
Bozitinib (PLB-1001) (PLB-1001) is a highly selective inhibitor of the c-MET kinase with blood-brain barrier permeability. Bozitinib binds to the conventional ATP-binding pocket of the tyrosine kinase superfamily. |
|
T8864 |
Thymidylate Kinase Inhibitor, YMU1
|
|
Others
|
|
YMU1 is a human thymidylate kinase (hTMPK) inhibitor. YMU1 stabilizes the conformation of ligand-induced degradation (LID) region of hTMPK and blocks the catalytic site or ATP-binding site. |
|
T15375 |
Inavolisib
|
GDC-0077,RG6114 |
Apoptosis
,
PI3K
|
|
Inavolisib (GDC-0077) is an orally available and selective inhibitor of PI3Kα (IC50=0.038 nM). Inavolisib is more selective for mutant versus wild-type PI3Kα. Inavolisib exerts its activity by binding to the ATP binding ... |
|
T6337 |
RepSox
|
ALK5 Inhibitor II,SJN 2511,E-616452 |
ALK
,
TGF-beta/Smad
|
|
RepSox (ALK5 Inhibitor II) is a TGFβR-1/ALK5 inhibitor that selectively inhibits the binding of ATP to ALK5 and the autophosphorylation of ALK5 (IC50=23/4 nM). RepSox induces adipogenesis in MEFs cells. |
|
T11348 |
G907
|
|
Antibiotic
|
|
G907 is a selective and potent antagonist of the small molecule ATP-binding cassette (ABC) transporter protein MsbA, with bactericidal activity, which traps MsbA in the inner lipopolysaccharide. G907 inhibits E. coli Msb... |
|
T3650 |
STO-609 acetate
|
|
CaMK
|
|
STO-609 acetate is selective, cell-permeable inhibitor of Ca2+-calmodulin-dependent protein kinase kinase (Ki: 80/15 ng/ml, for CaM-KKα/KKβ); competes for the ATP-binding site. It displays > 80-fold selectivity over CaMK... |
|
T4487 |
TNP
|
IP3K Inhibitor |
Others
|
|
TNP (IP3K Inhibitor) is a cell-permeable inhibitor of IP6K1 and IP3K, with IC 50 values of 0.55 μM and 10.2 μM for IP6K1 and IP3K, respectively. TNP binds to the ATP-binding sites of both enzymes [1]. |
|
T10965 |
DBPR112
|
|
EGFR
|
|
DBPR112 is an orally active furanopyrimidine-based EGFR inhibitor with IC50s of 15 nM and 48 nM for EGFRWT and EGFRL858R/T790M, respectively. DBPR112 can occupy the ATP-binding site. DBPR112 has significant antitumor eff... |
|
T7424 |
NDI-091143
|
|
ATP Citrate Lyase
|
|
NDI-091143 is a potent and high-affinity human ATP-citrate lyase (ACLY) inhibitor with an IC50 of 2.1 nM (ADP-Glo assay),indirectly disrupting citrate binding via an unexpected mechanism of inhibition. |
|
T16125 |
MMV390048
|
|
Parasite
,
PI4K
|
|
MMV390048 is an antimalarial agent and is a representative of a new chemical class of Plasmodium PI4K inhibitor (Kdapp=0.3 μM). MMV390048 binds to the ATP binding site of Plasmodium PI4K and does not bind to other P. fal... |
|
T1849 |
Momelotinib
|
CYT11387,CYT387,LM-1149 |
Apoptosis
,
JAK
,
Autophagy
|
|
Momelotinib (LM-1149) is an orally bioavailable small-molecule inhibitor of Janus kinases 1 and 2 (JAK1/2) with IC50 of 11 nM/18 nM. JAK1/2 inhibitor CYT387 competes with JAK1/2 for ATP binding, which may result in inhib... |
|
T14366 |
AZ10606120 dihydrochloride
|
|
P2X Receptor
|
|
AZ10606120 dihydrochloride is a selectable, potent, high-affinity receptor antagonist with K D values of 1.4 and 19 nM at human and rat P2X 7 receptors, respectively. AZ10606120 dihydrochloride inhibits tumor growth and ... |
|
T35343 |
MTI-31
|
MTI-31,LXI-15029 |
mTOR
|
|
MTI-31 (LXI-15029) is a potent, orally active and highly selective inhibitor of mTORC1 and mTORC2. MTI-31 is selective for mTOR (Kd: 0.20 nM) versus PIK3CA, PIK3CB and PIK3G with >5,000 fold selectivity in mTOR binding a... |
|
T2064 |
Semaxinib
|
SU5416 |
VEGFR
|
|
Semaxinib (SU5416) is a potent and selective VEGFR2 inhibitor (IC50: 1.23 μM), 20-fold more selective for VEGFR than PDGFRβ, lack of activity against InsR, EGFR, and FGFR. Semaxanib reversibly inhibits ATP binding to the... |
|
T17182 |
TX1-85-1
|
|
EGFR
|
|
TX1-85-1 induces partial degradation of Her3 protein and attenuates Her3-dependent signaling. TX1-85-1 is an irreversible Her3 inhibitor (IC50: 23 nM). TX1-85-1 is also the first selective Her3 ligand, which forms a cova... |
|
T16550 |
PKR-IN-C16
|
|
Others
|
|
PKR-IN-C16 is a specific protein kinase (PKR) inhibitor. PKR-IN-C16 is able to inhibit the autophosphorylation of PKR and unlock the translation blockade induced by PKR in primary neuronal cultures.PKR-IN-C16 binds the A... |
|
T8333 |
Aurintricarboxylic acid
|
ATA,NSC-4056,NSC4056,NSC 4056 |
Apoptosis
,
P2X Receptor
,
Influenza Virus
,
Topoisomerase
|
|
Aurintricarboxylic acid (NSC-4056) is a strong inhibitor of topoisomerases and other nucleases. It is a potent inhibitor of ribonuclease and topoisomerase II by preventing the binding of the nucleic acid to the enzyme. |
|
T2024 |
A-803467
|
A 803467,A803467 |
Sodium Channel
|
|
A-803467 is a selective NaV1.8 channel blocker. |
|
T1448L |
Dasatinib monohydrate
|
BMS-354825 Monohydrate |
Apoptosis
,
Bcr-Abl
,
Src
,
c-Kit
,
Ephrin Receptor
,
Autophagy
|
|
Dasatinib monohydrate (BMS-354825 Monohydrate) is an orally bioavailable synthetic small molecule-inhibitor of SRC-family protein-tyrosine kinases. Dasatinib monohydrate binds to and inhibits the growth-promoting activit... |
|
T23869 |
WEE1-IN-4
|
Wee1-Inhibitor-I,Wee1 Inhibitor-I,Wee1 Inhibitor I,Wee1-Inhibitor I |
|
|
Wee1 Inhibitor I is an ATP-binding site-targeting Wee1 inhibitor. |
|
T41113 |
3BrB-PP1
|
3BrB-PP1 |
|
|
3BrB-PP1 is an ATP-competitive analog that exhibits specific inhibitory activity towards protein kinase. It is effective in inhibiting protein kinase with mutations in the ATP-binding pocket, specifically the mutation of... |
|
T18917 |
ATP-Red 1
|
|
Others
|
|
ATP-Red 1 is a multisite-binding switchable fluorescent probe. It can rapidly and selectively respond to intracellular concentrations of ATP in living cells. |
|
T23881 |
Wee1 Inhibitor II
|
Wee1-Inhibitor II,Wee1-Inhibitor-II,Wee1 Inhibitor-II |
|
|
Wee1 Inhibitor II is an ATP-binding site-targeting Wee1 inhibitor. |
|
T28389 |
PF-6422899
|
PF6422899,PF 6422899 |
|
|
PF-6422899 irreversibly inhibits EGFR kinase activity by binding covalently to active-site cysteine residues in the ATP binding pocket of EGFR. |
|
T24098 |
GP17
|
GP-17,GP 17 |
|
|
GP17 is a type II kinase inhibitor of the IRE1α endoribonuclease that acts by targeting the ATP-binding pocket of IRE1α. |
|
T24099 |
GP29
|
GP-29,GP 29 |
|
|
GP29 is a Type II kinase inhibitor of the IRE1α endoribonuclease that acts by targeting the ATP-binding pocket of IRE1α. |
|
T36778 |
MK2-IN-1
|
MK2-IN-1 (MK2 Inhibitor) |
|
|
MK2-IN-1 is a potent and selecitve MAPKAPK2(MK2) inhibitor(IC50=0.11 uM) with a non-ATP competitive binding mode. |
|
T0373L1 |
Erlotinib mesylate
|
CP-358774,CP-358,774,OSI-774,CP358774,OSI 774 |
|
|
Erlotinib is an epidermal growth factor receptor inhibitor. Erlotinib binds in a reversible fashion to the adenosine triphosphate (ATP) binding site of the receptor. |
|
T32085 |
HM30181AK
|
HM-30181AK,HM 30181AK |
|
|
HM30181AK is an inhibitor of the adenosine triphosphate (ATP) binding cassette (ABC) transporter P-glycoprotein (P-gp) with adjuvant activity. |
|
T16107 |
ML230
|
CID44640177,SID 88095709 |
CGRP Receptor
|
|
ML230 is a selective ATP-binding cassette (ABC) transporter ABCG2 inhibitor. It 36-fold selective for ABCG2 over ABCB1 (EC50s: 0.13 μM and 4.65 μM, respectively). |
|
T74034 |
6-Me-ATP trisodium
|
|
|
|
6-Me-ATP (N6-Methyl-ATP) trisodium, an N6-modified ATP derivative, demonstrates high binding affinity for GSK3 and effectively acts as the phosphate group donor in GSK3β-catalyzed phosphorylation of its substrate peptide... |
|
T15659 |
KHK-IN-1 hydrochloride
|
|
Others
|
|
KHK-IN-1 hydrochloride is a potent inhibitor of ketohexokinase (KHK) (IC50: 12 nM). In the ATP-binding region of KHK, KHK-IN-1 hydrochloride interacts with Asp-27B. |
|
T68349 |
Lck inhibitor II
|
|
|
|
Lck inhibitor II is a cell-permeable, ATP binding site-targeting, tri-substituted pyrimidine that acts as a highly potent Lck (lymphocyte specific kinase) inhibitor |
|
T13547 |
AMP-PCP
|
|
HSP
|
|
AMP-PCP is an ATP analog and can bind to the Hsp90 N-terminal domain (Kd: 3.8 μM). AMP-PCP binding favors the formation of the active homodimer of Hsp90. |
|
T74033 |
6-Me-ATP
|
|
|
|
6-Me-ATP (N6-Methyl-ATP), a N6-modified adenosine triphosphate (ATP) derivative, exhibits strong binding affinity for glycogen synthase kinase 3 (GSK3) and acts as the phosphate group donor in GSK3β-catalyzed phosphoryla... |
|
T78832 |
FGFR1 inhibitor-9
|
|
FGFR
|
|
FGFR1 inhibitor-9 (Compound 7) is an FGFR1 inhibitor with potent binding affinity, exhibiting an IC50 of 0.85 nM. It targets the ATP-binding pocket of FGFR1 and demonstrates anticancer activity [1]. |
|
T33955 |
PF-6808472
|
OX-44,OX44,PF 6808472,OX 44,PF6808472 |
|
|
PF-6808472 is a cell permeable covalent probe suitable for click chemistry designated to measure kinase selectivity in intact cells. PF-6808472 contains sulfonyl fluoride group, which react with conserved lysine residue ... |
|
T62089 |
FWM-1
|
|
|
|
FWM-1 is a potent inhibitor of SARS-COV-2 NSP13 resolvase (free energy of binding: -328.6 kcal/mol).FWM-1 shows effective disruption of the binding of ATP to SARS-COV2 resolvase. |
|
T10172 |
5-Iodo-indirubin-3'-monoxime
|
|
GSK-3
,
CDK
|
|
5-Iodo-indirubin-3'-monoxime is a potent GSK-3β, CDK5/P25 and CDK1/cyclin B inhibitor, competing with ATP for binding to the catalytic site of the kinase (IC50s: 9, 20 and 25 nM). |
|
T78831 |
FGFR1 inhibitor-8
|
|
FGFR
|
|
FGFR1 inhibitor-8 (Compound 9), an FGFR1 inhibitor with an IC50 of 0.5 nM, binds to the ATP-binding pocket of FGFR1 and exhibits anticancer activity [1]. |
