General Information of the Protein
Protein ID
PT01441
Protein Name
Tyrosine-protein kinase SYK
Secondarily
Protein Name
Spleen tyrosine kinase
p72-Syk
Gene Name
SYK
Sequence
MASSGMADSANHLPFFFGNITREEAEDYLVQGGMSDGLYLLRQSRNYLGGFALSVAHGRKAHHYTIERELNGTYAIAGGRTHASPADLCHYHSQESDGLVCLLKKPFNRPQGVQPKTGPFEDLKENLIREYVKQTWNLQGQALEQAIISQKPQLEKLIATTAHEKMPWFHGKISREESEQIVLIGSKTNGKFLIRARDNNGSYALCLLHEGKVLHYRIDKDKTGKLSIPEGKKFDTLWQLVEHYSYKADGLLRVLTVPCQKIGTQGNVNFGGRPQLPGSHPATWSAGGIISRIKSYSFPKPGHRKSSPAQGNRQESTVSFNPYEPELAPWAADKGPQREALPMDTEVYESPYADPEEIRPKEVYLDRKLLTLEDKELGSGNFGTVKKGYYQMKKVVKTVAVKILKNEANDPALKDELLAEANVMQQLDNPYIVRMIGICEAESWMLVMEMAELGPLNKYLQQNRHVKDKNIIELVHQVSMGMKYLEESNFVHRDLAARNVLLVTQHYAKISDFGLSKALRADENYYKAQTHGKWPVKWYAPECINYYKFSSKSDVWSFGVLMWEAFSYGQKPYRGMKGSEVTAMLEKGERMGCPAGCPREMYDLMNLCWTYDVENRPGFAAVELRLRNYYYDVVN
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
TK protein kinase group
>
Tyrosine protein kinase Syk family
Function
Non-receptor tyrosine kinase which mediates signal transduction downstream of a variety of transmembrane receptors including classical immunoreceptors like the B-cell receptor (BCR). Regulates several biological processes including innate and adaptive immunity, cell adhesion, osteoclast maturation, platelet activation and vascular development (PubMed:12387735, PubMed:33782605). Assembles into signaling complexes with activated receptors at the plasma membrane via interaction between its SH2 domains and the receptor tyrosine-phosphorylated ITAM domains. The association with the receptor can also be indirect and mediated by adapter proteins containing ITAM or partial hemITAM domains. The phosphorylation of the ITAM domains is generally mediated by SRC subfamily kinases upon engagement of the receptor. More rarely signal transduction via SYK could be ITAM-independent. Direct downstream effectors phosphorylated by SYK include DEPTOR, VAV1, PLCG1, PI-3-kinase, LCP2 and BLNK (PubMed:12456653, PubMed:15388330, PubMed:8657103, PubMed:34634301). Initially identified as essential in B-cell receptor (BCR) signaling, it is necessary for the maturation of B-cells most probably at the pro-B to pre-B transition (PubMed:12456653). Activated upon BCR engagement, it phosphorylates and activates BLNK an adapter linking the activated BCR to downstream signaling adapters and effectors. It also phosphorylates and activates PLCG1 and the PKC signaling pathway. It also phosphorylates BTK and regulates its activity in B-cell antigen receptor (BCR)-coupled signaling. In addition to its function downstream of BCR also plays a role in T-cell receptor signaling. Plays also a crucial role in the innate immune response to fungal, bacterial and viral pathogens. It is for instance activated by the membrane lectin CLEC7A. Upon stimulation by fungal proteins, CLEC7A together with SYK activates immune cells inducing the production of ROS. Also activates the inflammasome and NF-kappa-B-mediated transcription of chemokines and cytokines in presence of pathogens. Regulates neutrophil degranulation and phagocytosis through activation of the MAPK signaling cascade (By similarity). Required for the stimulation of neutrophil phagocytosis by IL15 (PubMed:15123770). Also mediates the activation of dendritic cells by cell necrosis stimuli. Also involved in mast cells activation. Involved in interleukin-3/IL3-mediated signaling pathway in basophils (By similarity). Also functions downstream of receptors mediating cell adhesion (PubMed:12387735). Relays for instance, integrin-mediated neutrophils and macrophages activation and P-selectin receptor/SELPG-mediated recruitment of leukocytes to inflammatory loci. Also plays a role in non-immune processes. It is for instance involved in vascular development where it may regulate blood and lymphatic vascular separation. It is also required for osteoclast development and function. Functions in the activation of platelets by collagen, mediating PLCG2 phosphorylation and activation. May be coupled to the collagen receptor by the ITAM domain-containing FCER1G. Also activated by the membrane lectin CLEC1B that is required for activation of platelets by PDPN/podoplanin. Involved in platelet adhesion being activated by ITGB3 engaged by fibrinogen. Together with CEACAM20, enhances production of the cytokine CXCL8/IL-8 via the NFKB pathway and may thus have a role in the intestinal immune response (By similarity).
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Uniprot ID
P43405
Ensembl ID
ENSG00000165025
HGNC ID
HGNC:11491
Subcellular Location
Cell membrane
Cytoplasm
Cytosol
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000077 , Ba/F3
Compound ID Compound Name Compound Formula
CP0388620
methyl N-[4-[7-amino-3-(3,4-dimethoxyphenyl)-5-(1-methylpiperidin-4-yl)oxypyrazolo[1,5-a]pyrimidin-6-yl]phenyl]carbamate
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C28H32N6O5
 1
1
IC50 = 1400 nM
   TI
   LI
   LO
   TS
CP0418567
3-[4-amino-7-[3-(hydroxymethyl)cyclobutyl]pyrrolo[2,3-d]pyrimidin-5-yl]phenol
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C17H18N4O2
 1
1
IC50 = 2400 nM
   TI
   LI
   LO
   TS
CP0388864
4-[6-(benzylamino)imidazo[1,2-b]pyridazin-3-yl]benzonitrile
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C20H15N5
 1
1
IC50 = 4000 nM
   TI
   LI
   LO
   TS
CP0385508
2-[4-[4-[6-[(2R)-2-(3-fluorophenyl)pyrrolidin-1-yl]imidazo[1,2-b]pyridazin-3-yl]pyridin-2-yl]piperazin-1-yl]acetic acid
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C27H28FN7O2
 1
1
IC50 = 4400 nM
   TI
   LI
   LO
   TS
CP0061016
3-(4-Amino-7-cyclopentyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)-phenol
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C17H18N4O
 1
1
IC50 = 4900 nM
   TI
   LI
   LO
   TS
CP0661487
3-(2,6-Dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea monophosphate
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C26H34Cl2N7O7P
 1
1
IC50 = 5358 nM
   TI
   LI
   LO
   TS
CP0388616
3-(3,4-dimethoxyphenyl)-5-(1-methylpiperidin-4-yl)oxy-6-phenylpyrazolo[1,5-a]pyrimidin-7-amine
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C26H29N5O3
 1
1
IC50 = 7600 nM
   TI
   LI
   LO
   TS
CP0385511
1-[4-[6-[(2R)-2-(3-fluorophenyl)pyrrolidin-1-yl]imidazo[1,2-b]pyridazin-3-yl]pyridin-2-yl]piperidin-4-ol
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C26H27FN6O
 1
1
IC50 = 7900 nM
   TI
   LI
   LO
   TS
CP0388615
3-(3,4-dimethoxyphenyl)-5-(1-methylpiperidin-4-yl)oxy-6-(1,3-thiazol-2-yl)pyrazolo[1,5-a]pyrimidin-7-amine
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C23H26N6O3S
 1
1
IC50 > 11000 nM
   TI
   LI
   LO
   TS
CP0138866
1-[4-[3-[4-amino-5-(2-fluoro-5-hydroxyphenyl)pyrrolo[2,3-d]pyrimidin-7-yl]cyclobutyl]piperazin-1-yl]ethanone
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C22H25FN6O2
 1
1
IC50 > 11000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0117509
6-(6-aminopyrazin-2-yl)-N-(4-(4-(oxetan-3-yl)piperazin-1-yl)phenyl)imidazo[1,2-a]pyrazin-8-amine
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C23H25N9O
 4
1 EC50 = 90 nM
2 EC50 = 180 nM
3 EC50 = 700 nM
4 IC50 = 6.2 nM
CP0041572
BDBM50249542
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C22H23FN6O5
 8
1 EC50 = 111 nM
2 IC50 = 5.5 nM
3 IC50 = 23.62 nM
4 IC50 = 41 nM
5 IC50 = 64 nM
6 IC50 = 68 nM
7 Kd = 19 nM
8 Ki = 30 nM
CP0041751
US8871778, 141
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C22H24ClN7O
 2
1 IC50 = 0.03 nM
2 IC50 = 1 nM
CP0004106
(2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.1^{2,6}.0^{7,28}.0^{8,13}.0^{15,19}.0^{20,27}.0^{21,26}]nonacosa-8(13),9,11,14(28),15(19),20(27),21(26),22,24-nonaen-16-one
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C28H26N4O3
 11
1 IC50 < 0.1 nM
2 IC50 = 0.133 nM
3 IC50 = 0.217 nM
4 IC50 = 0.45 nM
5 IC50 < 1 nM
6 IC50 = 1.08 nM
7 IC50 = 1.3 nM
8 IC50 = 3 nM
9 IC50 = 60 nM
10 Kd = 7 nM
11 Kd = 14 nM
CP0090807
6-(1H-indazol-6-yl)-N-(3-methoxy-4-morpholin-4-ylphenyl)imidazo[1,2-a]pyrazin-8-amine
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C24H23N7O2
 1
1 IC50 = 0.44 nM
CP0574943
N-[4-(4-ethylpiperazin-1-yl)phenyl]-6-(1H-indazol-6-yl)imidazo[1,2-a]pyrazin-8-amine
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C25H26N8
 1
1 IC50 = 0.8 nM
CP0090813
4-[[3-[8-(3,4-dimethoxyanilino)imidazo[1,2-a]pyrazin-6-yl]benzoyl]amino]benzoic acid
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C28H23N5O5
 2
1 IC50 = 0.84 nM
2 Kd = 4 nM
CP0540766
6-(1H-indazol-6-yl)-N-[4-[4-(2-methoxyethyl)piperazin-1-yl]phenyl]imidazo[1,2-a]pyrazin-8-amine
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C26H28N8O
 1
1 IC50 = 0.9 nM
CP0823071
(R)-N-(4-(2-((dimethylamino)methyl)morpholino)phenyl)-6-(1H-indazol-6-yl)imidazo[1,2-a]pyrazin-8-amine
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C26H28N8O
 1
1 IC50 = 0.9 nM
CP0093554
BIIB-057
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C19H23N9O
 4
1 IC50 = 1 nM
2 IC50 = 6 nM
3 IC50 = 13 nM
4 IC50 = 540 nM
CP0165060
N-tert-butyl-2-[5-(difluoromethoxy)-1-methylindazol-3-yl]-5H-pyrrolo[2,3-b]pyrazine-7-carboxamide
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C20H20F2N6O2
 2
1 IC50 = 1 nM
2 IC50 = 2580 nM
CP0084714
7-[[(1R,2S)-2-aminocyclohexyl]amino]-5-(1H-indol-4-ylamino)-3H-pyrido[4,3-d]pyrimidin-4-one
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C21H23N7O
 1
1 IC50 = 1 nM
CP0084720
7-[[(3R,4R)-3-aminooxan-4-yl]amino]-5-[(3-methyl-1H-indol-7-yl)amino]-3H-pyrido[4,3-d]pyrimidin-4-one
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C21H23N7O2
 1
1 IC50 = 1 nM
CP0222796
6-[[(3R,4R)-3-aminooxan-4-yl]amino]-8-[(2-methylindazol-4-yl)amino]-2H-2,7-naphthyridin-1-one
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C21H23N7O2
 1
1 IC50 = 1 nM
CP0245877
5-[[(1R,2S)-2-aminocyclohexyl]amino]-3-[3-(triazol-2-yl)anilino]pyrazine-2-carboxamide
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C19H23N9O
 1
1 IC50 = 1 nM
CP0722967
5-(1H-indol-4-ylamino)-3-((1R,2S)-2-aminocyclohexylamino)-1,2,4-triazine-6-carboxamide
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C18H22N8O
 1
1 IC50 = 1 nM
CP0095342
US8871778, 189
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C23H26ClN7O
 1
1 IC50 = 1 nM
CP0834359
(R)-(4-(4-((6-(1H-indazol-6-yl)imidazo[1,2-a]pyrazin-8-yl)amino)phenyl)morpholin-2-yl)methanol
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C24H23N7O2
 1
1 IC50 = 1.1 nM
CP0368580
1-[4-[[6-(1H-indazol-6-yl)imidazo[1,2-a]pyrazin-8-yl]amino]phenyl]piperidin-4-ol
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C24H23N7O
 1
1 IC50 = 1.2 nM
CP0131482
1-[4-[[6-(1H-indazol-6-yl)imidazo[1,2-a]pyrazin-8-yl]amino]phenyl]-4-methylpiperidin-4-ol
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C25H25N7O
 1
1 IC50 = 1.4 nM
CP0399155
3-[8-(3,4-dimethoxyanilino)imidazo[1,2-a]pyrazin-6-yl]-N-[4-(1H-tetrazol-5-yl)phenyl]benzamide
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C28H23N9O3
 1
1 IC50 = 1.5 nM
CP0095252
1-[[3-methyl-1-[2-[(1,2,3-trimethylindol-5-yl)amino]pyrimidin-4-yl]pyrazol-4-yl]methyl]azetidin-3-ol
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C23H27N7O
 1
1 IC50 = 1.7 nM
CP0368581
N-[4-[4-(oxetan-3-yl)piperazin-1-yl]phenyl]-6-(5H-pyrrolo[2,3-b]pyrazin-3-yl)imidazo[1,2-a]pyrazin-8-amine
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C25H25N9O
 1
1 IC50 = 1.7 nM
CP0131336
N-tert-butyl-2-[5-(difluoromethoxy)-1H-indazol-3-yl]-5H-pyrrolo[2,3-b]pyrazine-7-carboxamide
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C19H18F2N6O2
 2
1 IC50 = 2 nM
2 IC50 = 2450 nM
CP0188380
N-tert-butyl-2-[5-(difluoromethoxy)-1-(3,4-dihydroxybutyl)indazol-3-yl]-5H-pyrrolo[2,3-b]pyrazine-7-carboxamide
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C23H26F2N6O4
 2
1 IC50 = 2 nM
2 IC50 = 534 nM
CP0084716
7-[[(1R,2S)-2-aminocyclohexyl]amino]-5-[(3-methyl-1H-indol-7-yl)amino]-3H-pyrido[4,3-d]pyrimidin-4-one
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C22H25N7O
 1
1 IC50 = 2 nM
CP0125451
N-[4-(1,1-dioxo-1,4-thiazinan-4-yl)phenyl]-6-(1H-indazol-6-yl)imidazo[1,2-a]pyrazin-8-amine
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C23H21N7O2S
 2
1 IC50 = 2.1 nM
2 IC50 = 19.5 nM
CP0090802
3-[8-(3,4-dimethoxyanilino)imidazo[1,2-a]pyrazin-6-yl]-N-[4-(methylsulfonylcarbamoyl)phenyl]benzamide
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C29H26N6O6S
 1
1 IC50 = 2.2 nM
CP0397359
6-[8-(3,4-dimethoxyanilino)imidazo[1,2-a]pyrazin-6-yl]-4H-1,4-benzoxazin-3-one
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C22H19N5O4
 1
1 IC50 = 2.3 nM
CP0177722
(3R)-1-[[1-[2-(3,5-dimethylanilino)pyrimidin-4-yl]-4-methylpyrrol-3-yl]methyl]pyrrolidin-3-ol
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C22H27N5O
 1
1 IC50 = 2.3 nM
CP0434793
2-[4-[[3-[8-(3,4-dimethoxyanilino)imidazo[1,2-a]pyrazin-6-yl]benzoyl]amino]phenyl]acetic acid
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C29H25N5O5
 1
1 IC50 = 2.6 nM
CP0399157
N-(3,4-dimethoxyphenyl)-6-(1H-indol-6-yl)imidazo[1,2-a]pyrazin-8-amine
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C22H19N5O2
 1
1 IC50 = 2.7 nM
CP0547574
N-[4-[4-(oxetan-3-yl)piperazin-1-yl]phenyl]-6-(1H-pyrazolo[4,3-b]pyridin-6-yl)imidazo[1,2-a]pyrazin-8-amine
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C25H25N9O
 1
1 IC50 = 2.8 nM
CP0131329
N-tert-butyl-2-[5-(difluoromethoxy)-1-(3-morpholin-4-ylpropyl)indazol-3-yl]-5H-pyrrolo[2,3-b]pyrazine-7-carboxamide
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C26H31F2N7O3
 2
1 IC50 = 3 nM
2 IC50 = 277 nM
CP0131333
N-tert-butyl-2-[7-(hydroxymethyl)-2H-indazol-3-yl]-5H-pyrrolo[2,3-b]pyrazine-7-carboxamide
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C19H20N6O2
 2
1 IC50 = 3 nM
2 IC50 = 412 nM
CP0189631
N-tert-butyl-2-[5-(difluoromethoxy)-1-(3-methylsulfonylpropyl)indazol-3-yl]-5H-pyrrolo[2,3-b]pyrazine-7-carboxamide
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C23H26F2N6O4S
 2
1 IC50 = 3 nM
2 IC50 = 335 nM
CP0183356
6-[[(1R,2S)-2-aminocyclohexyl]amino]-8-[(3-methyl-1H-indol-7-yl)amino]-2H-2,7-naphthyridin-1-one
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C23H26N6O
 1
1 IC50 = 3 nM
CP0323205
N-[4-[4-(oxetan-3-yl)piperazin-1-yl]phenyl]-6-(1H-pyrazolo[3,4-b]pyrazin-6-yl)imidazo[1,2-a]pyrazin-8-amine
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C24H24N10O
 1
1 IC50 = 3.2 nM
CP0093068
N-(3,4-dimethoxyphenyl)-6-(1H-indazol-6-yl)imidazo[1,2-a]pyrazin-8-amine
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C21H18N6O2
 2
1 IC50 = 3.8 nM
2 Kd = 9 nM
CP0093069
6-(1H-indazol-6-yl)-N-[4-(oxan-4-yl)phenyl]imidazo[1,2-a]pyrazin-8-amine
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C24H22N6O
 1
1 IC50 = 3.8 nM
CP0399159
1-[4-[[6-(1H-indazol-6-yl)imidazo[1,2-a]pyrazin-8-yl]amino]phenyl]-3-methylazetidin-3-ol
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C23H21N7O
 1
1 IC50 = 3.9 nM
CP0105423
5-((1S,2R)-2-aminocyclohexylamino)-7-(3,5-dimethoxyphenylamino)-[1,2,4]triazolo[1,5-c]pyrimidine-8-carboxamide
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C20H26N8O3
 1
1 IC50 = 4 nM
CP0131600
CHEMBL2347413
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C20H20FN7O
 2
1 IC50 = 4 nM
2 IC50 = 581 nM
CP0165059
N-tert-butyl-2-(6-fluoro-1-piperidin-4-ylindazol-3-yl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxamide
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C23H26FN7O
 2
1 IC50 = 4 nM
2 IC50 = 852 nM
CP0189636
N-tert-butyl-2-[1-[3-(3-cyanoazetidin-1-yl)propyl]-5-(difluoromethoxy)indazol-3-yl]-5H-pyrrolo[2,3-b]pyrazine-7-carboxamide
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C26H28F2N8O2
 2
1 IC50 = 4 nM
2 IC50 = 534 nM
CP0316189
N-tert-butyl-2-(6-fluoro-1-methylindazol-3-yl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxamide
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C19H19FN6O
 1
1 IC50 = 4 nM
CP0118574
7-[[(1R,2S)-2-aminocyclohexyl]amino]-5-(1H-indol-7-ylamino)-3H-pyrido[4,3-d]pyrimidin-4-one
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C21H23N7O
 1
1 IC50 = 4 nM
CP0118577
6-[[(1R,2S)-2-aminocyclohexyl]amino]-8-[(3-chloro-1H-indol-7-yl)amino]-2H-2,7-naphthyridin-1-one
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C22H23ClN6O
 1
1 IC50 = 4 nM
CP0117949
2-[2-(1H-thieno[3,2-c]pyrazol-3-yl)-1H-indol-6-yl]propan-2-ol
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C16H15N3OS
 1
1 IC50 = 4 nM
CP0090801
N-(4-carbamoylphenyl)-3-[8-(3,4-dimethoxyanilino)imidazo[1,2-a]pyrazin-6-yl]benzamide
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C28H24N6O4
 1
1 IC50 = 4.3 nM
CP0395436
6-(3,4-dihydro-2H-1,4-benzoxazin-6-yl)-N-(3,4-dimethoxyphenyl)imidazo[1,2-a]pyrazin-8-amine
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C22H21N5O3
 1
1 IC50 = 4.7 nM
CP0965358
N-(4-((2S,6R)-2,6-dimethylmorpholino)phenyl)-6-(1H-indazol-6-yl)imidazo[1,2-a]pyrazin-8-amine
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C25H25N7O
 1
1 IC50 = 4.9 nM
CP0131328
N-tert-butyl-2-[1-(3,4-dihydroxybutyl)-6-fluoroindazol-3-yl]-5H-pyrrolo[2,3-b]pyrazine-7-carboxamide
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C22H25FN6O3
 2
1 IC50 = 5 nM
2 IC50 = 360 nM
CP0131599
N-tert-butyl-2-[5-(hydroxymethyl)-1-methylindazol-3-yl]-5H-pyrrolo[2,3-b]pyrazine-7-carboxamide
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C20H22N6O2
 2
1 IC50 = 5 nM
2 IC50 = 839 nM
CP0180795
N-tert-butyl-2-[6-fluoro-1-(3-methylsulfonylpropyl)indazol-3-yl]-5H-pyrrolo[2,3-b]pyrazine-7-carboxamide
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C22H25FN6O3S
 2
1 IC50 = 5 nM
2 IC50 = 285 nM
CP0302172
N-tert-butyl-2-[5-(difluoromethoxy)-1-[3-(dimethylamino)propyl]indazol-3-yl]-5H-pyrrolo[2,3-b]pyrazine-7-carboxamide
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C24H29F2N7O2
 2
1 IC50 = 5 nM
2 IC50 = 184 nM
CP0183360
7-[[(1R,2S)-2-aminocyclohexyl]amino]-5-[3-(triazol-2-yl)anilino]-3H-pyrido[4,3-d]pyrimidin-4-one
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C21H23N9O
 1
1 IC50 = 5 nM
CP0365726
3-[[(1R,2S)-2-aminocyclohexyl]amino]-5-[3-(triazol-2-yl)anilino]-1,2,4-triazine-6-carboxamide
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C18H22N10O
 1
1 IC50 = 5 nM
CP0761533
3-(1H-indol-7-ylamino)-5-((1R,2S)-2-aminocyclohexylamino)pyrazine-2-carboxamide
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C19H23N7O
 1
1 IC50 = 5 nM
CP0185405
(4R)-4-[(1R)-1-[[6-(3,4-dimethoxyphenyl)-[1,3]thiazolo[5,4-c]pyridin-4-yl]oxy]ethyl]pyrrolidin-2-one
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C20H21N3O4S
 1
1 IC50 = 5 nM
CP0267292
8-[[4-(cyclopropylamino)furo[3,2-d]pyrimidin-2-yl]amino]-5,5-dimethyl-3,4-dihydro-1H-1-benzazepin-2-one
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C21H23N5O2
 1
1 IC50 = 5 nM
CP0562819
8-[[4-(cyclopropylamino)furo[3,2-d]pyrimidin-2-yl]amino]-5,5-dimethyl-1H-4,1-benzoxazepin-2-one
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C20H21N5O3
 1
1 IC50 = 5 nM
CP0570055
6-(1H-indazol-6-yl)-N-[4-(2-oxa-6-azaspiro[3.3]heptan-6-yl)phenyl]imidazo[1,2-a]pyrazin-8-amine
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C24H21N7O
 1
1 IC50 = 5 nM
CP0694111
N-(4-((1S,4S)-2-oxa-5-azabicyclo[2.2.1]heptan-5-yl)phenyl)-6-(1H-indazol-6-yl)imidazo[1,2-a]pyrazin-8-amine
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C24H21N7O
 1
1 IC50 = 5 nM
CP0948350
N-(4-((1R,5S)-8-oxa-3-azabicyclo[3.2.1]octan-3-yl)phenyl)-6-(1H-indazol-6-yl)imidazo[1,2-a]pyrazin-8-amine
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C25H23N7O
 1
1 IC50 = 5.3 nM
CP0244926
2-(6-chloro-1-methylindazol-3-yl)-N-(1-hydroxy-2-methylpropan-2-yl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxamide
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C19H19ClN6O2
 2
1 IC50 = 6 nM
2 IC50 = 6480 nM
CP0238205
8-[[4-(ethylamino)furo[3,2-d]pyrimidin-2-yl]amino]-5,5-dimethyl-1H-4,1-benzoxazepin-2-one
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C19H21N5O3
 1
1 IC50 = 6 nM
CP0415816
6-(3H-benzimidazol-5-yl)-N-(3,4-dimethoxyphenyl)imidazo[1,2-a]pyrazin-8-amine
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C21H18N6O2
 1
1 IC50 = 6.3 nM
CP0125698
N-[4-[4-(oxetan-3-yl)piperazin-1-yl]phenyl]-6-(1H-pyrazolo[3,4-b]pyridin-6-yl)imidazo[1,2-a]pyrazin-8-amine
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C25H25N9O
 1
1 IC50 = 6.7 nM
CP0570056
N-[4-[4-(oxetan-3-yl)piperazin-1-yl]phenyl]-6-(1H-pyrrolo[3,2-b]pyridin-6-yl)imidazo[1,2-a]pyrazin-8-amine
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C26H26N8O
 1
1 IC50 = 6.9 nM
CP0282163
4-[[3-[7-(3,4-dimethoxyanilino)-[1,3]thiazolo[5,4-d]pyrimidin-5-yl]benzoyl]amino]benzoic acid
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C27H21N5O5S
 2
1 IC50 = 7 nM
2 IC50 = 11900 nM
CP0131338
N-tert-butyl-2-(6-chloro-1-methylindazol-3-yl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxamide
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C19H19ClN6O
 2
1 IC50 = 7 nM
2 IC50 > 50000 nM
CP0059737
6-(1H-indazol-6-yl)-N-(4-methoxyphenyl)imidazo[1,2-a]pyrazin-8-amine
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C20H16N6O
 1
1 IC50 = 7 nM
CP0081059
5,5-dimethyl-8-[[4-(2,2,2-trifluoroethylamino)furo[3,2-d]pyrimidin-2-yl]amino]-1H-4,1-benzoxazepin-2-one
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C19H18F3N5O3
 2
1 IC50 = 7 nM
2 IC50 = 9 nM
CP0090806
2-[4-[[6-(1H-indazol-6-yl)imidazo[1,2-a]pyrazin-8-yl]amino]-N-methylanilino]ethanol
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C22H21N7O
 1
1 IC50 = 7.6 nM
CP0057741
6-(1H-indazol-6-yl)-N-(4-morpholin-4-ylphenyl)imidazo[1,2-a]pyrazin-8-amine
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C23H21N7O
 6
1 IC50 = 7.7 nM
2 IC50 = 11 nM
3 IC50 = 16.5 nM
4 IC50 = 82 nM
5 IC50 = 147 nM
6 IC50 = 377 nM
CP0525503
6-(3,4-dihydro-2H-pyrazino[2,3-b][1,4]oxazin-6-yl)-N-[4-[4-(oxetan-3-yl)piperazin-1-yl]phenyl]imidazo[1,2-a]pyrazin-8-amine
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C25H27N9O2
 1
1 IC50 = 7.8 nM
CP0400103
3-[5-(5-ethoxy-6-fluoro-1H-benzimidazol-2-yl)-1H-pyrazol-4-yl]-1,1-diethylurea
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C17H21FN6O2
 1
1 IC50 = 8 nM
CP0127635
6-(2,3-dihydro-1H-pyrido[2,3-b][1,4]oxazin-7-yl)-N-[4-[4-(oxetan-3-yl)piperazin-1-yl]phenyl]imidazo[1,2-a]pyrazin-8-amine
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C26H28N8O2
 1
1 IC50 = 8.4 nM
CP0399158
6-(1H-indazol-6-yl)-N-(3-methoxyphenyl)imidazo[1,2-a]pyrazin-8-amine
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C20H16N6O
 1
1 IC50 = 8.5 nM
CP0057732
N-(3,4-dimethoxyphenyl)-6-(1H-indol-5-yl)imidazo[1,2-a]pyrazin-8-amine
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C22H19N5O2
 1
1 IC50 = 8.6 nM
CP0093067
3-[[3-[8-(3,4-dimethoxyanilino)imidazo[1,2-a]pyrazin-6-yl]benzoyl]amino]benzoic acid
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C28H23N5O5
 1
1 IC50 = 8.9 nM
CP0163895
5-((1S,2R)-2-aminocyclohexylamino)-7-(3,5-dimethoxyphenylamino)-[1,2,4]triazolo[4,3-c]pyrimidine-8-carboxamide
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C20H26N8O3
 1
1 IC50 = 9 nM
CP0147657
(5R)-5-[(1R)-1-[[5-[1-(difluoromethyl)pyrazol-4-yl]-1,3-benzothiazol-7-yl]oxy]ethyl]-1,3-oxazolidin-2-one
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C16H14F2N4O3S
 1
1 IC50 = 9 nM
CP0127634
6-(1H-indazol-6-yl)-N-[4-(7-oxa-2-azaspiro[3.5]nonan-2-yl)phenyl]imidazo[1,2-a]pyrazin-8-amine
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C26H25N7O
 1
1 IC50 = 9 nM
CP0329990
6-(1H-indazol-6-yl)-N-[4-[4-(oxetan-3-yl)piperazin-1-yl]phenyl]imidazo[1,2-a]pyrazin-8-amine
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C26H26N8O
 1
1 IC50 = 9.2 nM
CP0940632
6-(1H-indazol-6-yl)-N-(4-(tetrahydro-1H-furo[3,4-c]pyrrol-5(3H)-yl)phenyl)imidazo[1,2-a]pyrazin-8-amine
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C25H23N7O
 1
1 IC50 = 9.6 nM
CP0131332
N-tert-butyl-2-[7-(2-hydroxypropan-2-yl)-2H-indazol-3-yl]-5H-pyrrolo[2,3-b]pyrazine-7-carboxamide
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C21H24N6O2
 2
1 IC50 = 10 nM
2 IC50 = 534 nM
CP0246641
CHEMBL2347414
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C20H20FN7O
 2
1 IC50 = 10 nM
2 IC50 = 427 nM
CP0169426
N-(3,4-dimethoxyphenyl)-6-(1H-indazol-5-yl)imidazo[1,2-a]pyrazin-8-amine
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C21H18N6O2
 1
1 IC50 = 10.4 nM
CP0114932
3-[8-(3,4-dimethoxyanilino)imidazo[1,2-a]pyrazin-6-yl]-N-[4-(1H-pyrazol-4-yl)phenyl]benzamide
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C30H25N7O3
 1
1 IC50 = 11 nM
CP0323206
N-[4-[4-(oxetan-3-yl)piperazin-1-yl]phenyl]-6-(1H-pyrrolo[2,3-b]pyridin-6-yl)imidazo[1,2-a]pyrazin-8-amine
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C26H26N8O
 1
1 IC50 = 11.3 nM
CP0525500
1-[4-[[6-(1H-indazol-6-yl)imidazo[1,2-a]pyrazin-8-yl]amino]phenyl]azetidin-3-ol
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C22H19N7O
 1
1 IC50 = 11.3 nM
CP0329992
6-(3H-imidazo[4,5-b]pyrazin-5-yl)-N-[4-[4-(oxetan-3-yl)piperazin-1-yl]phenyl]imidazo[1,2-a]pyrazin-8-amine
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C24H24N10O
 1
1 IC50 = 11.5 nM
CP0169423
3-[8-(3,4-dimethoxyanilino)imidazo[1,2-a]pyrazin-6-yl]-N-[4-(1H-pyrazol-3-yl)phenyl]benzamide
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C30H25N7O3
 1
1 IC50 = 11.7 nM
CP0314386
methyl N-[(3R)-8-[[4-(cyclopropylamino)furo[3,2-d]pyrimidin-2-yl]amino]-5,5-dimethyl-2-oxo-3,4-dihydro-1H-1-benzazepin-3-yl]carbamate
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C23H26N6O4
 1
1 IC50 = 12 nM
CP0090805
N-(3,4-dimethoxyphenyl)-6-(1-methylindazol-6-yl)imidazo[1,2-a]pyrazin-8-amine
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C22H20N6O2
 1
1 IC50 = 12.3 nM
CP0131480
6-(2H-benzotriazol-5-yl)-N-(3,4-dimethoxyphenyl)imidazo[1,2-a]pyrazin-8-amine
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C20H17N7O2
 1
1 IC50 = 12.6 nM
CP0337846
2-(6-chloro-1-methylindazol-3-yl)-N-[(2S)-1-hydroxypropan-2-yl]-5H-pyrrolo[2,3-b]pyrazine-7-carboxamide
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C18H17ClN6O2
 2
1 IC50 = 13 nM
2 IC50 = 4850 nM
CP0122057
5,5-dimethyl-8-[[4-(propan-2-ylamino)furo[3,2-d]pyrimidin-2-yl]amino]-1H-4,1-benzoxazepin-2-one
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C20H23N5O3
 1
1 IC50 = 13 nM
CP0329991
6-(1H-imidazo[4,5-b]pyridin-6-yl)-N-[4-[4-(oxetan-3-yl)piperazin-1-yl]phenyl]imidazo[1,2-a]pyrazin-8-amine
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C25H25N9O
 1
1 IC50 = 13.4 nM
CP0834358
N-(4-((1s,5s)-3,7-dioxa-9-azabicyclo[3.3.1]nonan-9-yl)phenyl)-6-(1H-indazol-6-yl)imidazo[1,2-a]pyrazin-8-amine
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C25H23N7O2
 1
1 IC50 = 13.7 nM
CP0165061
N-propan-2-yl-2-(3,4,5-trimethoxyphenyl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxamide
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C19H22N4O4
 2
1 IC50 = 14 nM
2 IC50 = 7090 nM
CP0131477
methyl 4-[[3-[8-(3,4-dimethoxyanilino)imidazo[1,2-a]pyrazin-6-yl]benzoyl]amino]benzoate
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C29H25N5O5
 1
1 IC50 = 15.2 nM
CP0558177
6-(1H-indol-6-yl)-N-[4-[4-(oxetan-3-yl)piperazin-1-yl]phenyl]imidazo[1,2-a]pyrazin-8-amine
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C27H27N7O
 1
1 IC50 = 15.7 nM
CP0138682
2-[6-fluoro-1-(3-methylsulfonylpropyl)indazol-3-yl]-N-(1-hydroxy-2-methylpropan-2-yl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxamide
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C22H25FN6O4S
 2
1 IC50 = 16 nM
2 IC50 = 94 nM
CP0116183
(5R)-5-[(1R)-1-[[6-[1-(difluoromethyl)pyrazol-4-yl]-2,1-benzothiazol-4-yl]oxy]ethyl]-1,3-oxazolidin-2-one
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C16H14F2N4O3S
 1
1 IC50 = 16 nM
CP0176762
(5R)-5-[(1R)-1-[[6-(1-methylpyrazol-4-yl)-2,1-benzothiazol-4-yl]oxy]ethyl]-1,3-oxazolidin-2-one
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C16H16N4O3S
 1
1 IC50 = 16 nM
CP0090803
3-[8-(3,4-dimethoxyanilino)imidazo[1,2-a]pyrazin-6-yl]-N-[4-(1H-imidazol-2-yl)phenyl]benzamide
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C30H25N7O3
 1
1 IC50 = 16.5 nM
CP0131605
FOSTAMATINIB
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C23H26FN6O9P
 2
1 IC50 = 17 nM
2 IC50 = 12000 nM
CP0559741
6-(3H-benzimidazol-5-yl)-N-[4-[4-(oxetan-3-yl)piperazin-1-yl]phenyl]imidazo[1,2-a]pyrazin-8-amine
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C26H26N8O
 1
1 IC50 = 17.3 nM
CP0557399
4-[8-(3,4-dimethoxyanilino)imidazo[1,2-a]pyrazin-6-yl]benzamide
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C21H19N5O3
 1
1 IC50 = 17.7 nM
CP0169425
4-[8-(3,4-dimethoxyanilino)imidazo[1,2-a]pyrazin-6-yl]-2-fluorobenzamide
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C21H18FN5O3
 1
1 IC50 = 18.6 nM
CP0131595
N-tert-butyl-2-[5-(difluoromethoxy)-1-[(1-methylazetidin-3-yl)methyl]indazol-3-yl]-5H-pyrrolo[2,3-b]pyrazine-7-carboxamide
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C24H27F2N7O2
 2
1 IC50 = 19 nM
2 IC50 = 546 nM
CP0121931
6-[[(1R,2S)-2-aminocyclohexyl]amino]-2-[3-(triazol-2-yl)anilino]pyridine-3-carboxamide
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C20H24N8O
 1
1 IC50 = 19 nM
CP0084717
7-[[(3R,4R)-3-aminooxan-4-yl]amino]-5-(1H-indol-7-ylamino)-3H-pyrido[4,3-d]pyrimidin-4-one
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C20H21N7O2
 1
1 IC50 = 20 nM
CP0122058
methyl N-[(3R)-8-[[4-(2,2-difluoroethylamino)furo[3,2-d]pyrimidin-2-yl]amino]-5,5-dimethyl-2-oxo-3,4-dihydro-1H-1-benzazepin-3-yl]carbamate
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C22H24F2N6O4
 1
1 IC50 = 20 nM
CP0169427
N-(3,4-dimethoxyphenyl)-6-(1-methylindazol-5-yl)imidazo[1,2-a]pyrazin-8-amine
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C22H20N6O2
 1
1 IC50 = 20.9 nM
CP0084719
7-[[(2S)-2-aminopropyl]amino]-5-(1H-indol-7-ylamino)-3H-pyrido[4,3-d]pyrimidin-4-one
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C18H19N7O
 1
1 IC50 = 21 nM
CP0342413
6-(3,4-dihydro-2H-1,4-benzoxazin-6-yl)-N-[4-[4-(oxetan-3-yl)piperazin-1-yl]phenyl]imidazo[1,2-a]pyrazin-8-amine
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C27H29N7O2
 1
1 IC50 = 21.5 nM
CP0183353
6-[[(3R,4R)-3-aminooxan-4-yl]amino]-8-(1H-indol-7-ylamino)-2H-2,7-naphthyridin-1-one
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C21H22N6O2
 1
1 IC50 = 22 nM
CP0081062
4-N-cyclopropyl-2-N-(3-methyl-2H-indazol-6-yl)furo[3,2-d]pyrimidine-2,4-diamine
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C17H16N6O
 2
1 IC50 = 23 nM
2 IC50 = 24 nM
CP0419327
6-(1H-indazol-6-yl)-N-[4-(1,4-oxazepan-4-yl)phenyl]imidazo[1,2-a]pyrazin-8-amine
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C24H23N7O
 1
1 IC50 = 23.1 nM
CP0381549
4-[8-(3,4-dimethoxyanilino)imidazo[1,2-a]pyrazin-6-yl]-2-methoxybenzamide
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C22H21N5O4
 1
1 IC50 = 23.8 nM
CP0131614
2-(6-chloroindazol-1-yl)-N-(1-hydroxy-2-methylpropan-2-yl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxamide
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C18H17ClN6O2
 2
1 IC50 = 24 nM
2 IC50 = 9950 nM
CP0251299
N-tert-butyl-2-(5,6,7,8-tetrahydroimidazo[1,5-a]pyridin-1-yl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxamide
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C18H22N6O
 2
1 IC50 = 26 nM
2 IC50 = 634 nM
CP0233502
(4R)-4-[(1R)-1-[[6-(1-methylpyrazol-4-yl)-[1,3]thiazolo[5,4-c]pyridin-4-yl]oxy]ethyl]pyrrolidin-2-one
   Show/Hide
C16H17N5O2S
 1
1 IC50 = 26 nM
CP0397360
6-(1H-indazol-6-yl)-N-phenylimidazo[1,2-a]pyrazin-8-amine
   Show/Hide
C19H14N6
 1
1 IC50 = 26.8 nM
CP0558836
3-[8-(3,4-dimethoxyanilino)imidazo[1,2-a]pyrazin-6-yl]benzamide
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C21H19N5O3
 1
1 IC50 = 27.1 nM
CP0399156
5-[8-(3,4-dimethoxyanilino)imidazo[1,2-a]pyrazin-6-yl]-2-methylbenzamide
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C22H21N5O3
 1
1 IC50 = 28.3 nM
CP0127636
6-(5-aminopyridin-3-yl)-N-[4-[4-(oxetan-3-yl)piperazin-1-yl]phenyl]imidazo[1,2-a]pyrazin-8-amine
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C24H26N8O
 1
1 IC50 = 28.6 nM
CP0138683
2-[5-(difluoromethoxy)-1-[3-(dimethylamino)propyl]indazol-3-yl]-N-(1-hydroxy-2-methylpropan-2-yl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxamide
   Show/Hide
C24H29F2N7O3
 2
1 IC50 = 30 nM
2 IC50 = 101 nM
CP0368619
6-(1H-imidazo[4,5-b]pyridin-5-yl)-N-[4-[4-(oxetan-3-yl)piperazin-1-yl]phenyl]imidazo[1,2-a]pyrazin-8-amine
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C25H25N9O
 1
1 IC50 = 31.9 nM
CP0337854
N-tert-butyl-2-(6-methoxyindazol-1-yl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxamide
   Show/Hide
C19H20N6O2
 1
1 IC50 = 33 nM
CP0094511
(4R)-4-[(1R)-1-[[5-(1-methylpyrazol-4-yl)-1,3-benzothiazol-7-yl]oxy]ethyl]pyrrolidin-2-one
   Show/Hide
C17H18N4O2S
 1
1 IC50 = 33 nM
CP0558967
7-[8-(3,4-dimethoxyanilino)imidazo[1,2-a]pyrazin-6-yl]-4H-1,4-benzoxazin-3-one
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C22H19N5O4
 1
1 IC50 = 33.4 nM
CP0095465
N'-[7-[4-(dimethylamino)phenyl]-1,6-naphthyridin-5-yl]propane-1,3-diamine
   Show/Hide
C19H23N5
 2
1 IC50 = 34 nM
2 IC50 = 552 nM
CP0131597
2-(1,6-dimethylindazol-3-yl)-N-(3-methylpyrrolidin-3-yl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxamide
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C21H23N7O
 2
1 IC50 = 34 nM
2 IC50 = 1770 nM
CP0183352
7-[[(1R,2S)-2-aminocyclohexyl]amino]-5-[(3-chloro-1H-indol-7-yl)amino]-3H-pyrido[4,3-d]pyrimidin-4-one
   Show/Hide
C21H22ClN7O
 1
1 IC50 = 34 nM
CP0131603
2-(3,4-dimethoxyphenyl)-N-(1-hydroxypropan-2-yl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxamide
   Show/Hide
C18H20N4O4
 2
1 IC50 = 35 nM
2 IC50 = 911 nM
CP0658097
5-(1H-indol-7-ylamino)-3-((1R,2S)-2-aminocyclohexylamino)-1,2,4-triazine-6-carboxamide
   Show/Hide
C18H22N8O
 2
1 IC50 = 35 nM
2 Kd = 0.64 nM
CP0159500
2-(6-chloro-1-methylindazol-3-yl)-N-propan-2-yl-5H-pyrrolo[2,3-b]pyrazine-7-carboxamide
   Show/Hide
C18H17ClN6O
 2
1 IC50 = 36 nM
2 IC50 = 16600 nM
CP0558993
5-[8-(3,4-dimethoxyanilino)imidazo[1,2-a]pyrazin-6-yl]-2-methoxybenzamide
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C22H21N5O4
 1
1 IC50 = 37.4 nM
CP0066654
(5R)-5-[(1R)-1-[[6-[1-(difluoromethyl)pyrazol-4-yl]-[1,3]thiazolo[5,4-c]pyridin-4-yl]oxy]ethyl]-1,3-oxazolidin-2-one
   Show/Hide
C15H13F2N5O3S
 1
1 IC50 = 38 nM
CP0095463
(4R)-4-[(1R)-1-[[6-(1-methylpyrazol-4-yl)-[1,2]thiazolo[4,3-c]pyridin-4-yl]oxy]ethyl]pyrrolidin-2-one
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C16H17N5O2S
 1
1 IC50 = 40 nM
CP0546652
5,5-dimethyl-8-[[4-(2,2,2-trifluoroethylamino)furo[3,2-d]pyrimidin-2-yl]amino]-3,4-dihydro-1H-1-benzazepin-2-one
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C20H20F3N5O2
 1
1 IC50 = 43 nM
CP0342414
6-(3,4-dihydro-2H-pyrido[3,2-b][1,4]oxazin-6-yl)-N-[4-[4-(oxetan-3-yl)piperazin-1-yl]phenyl]imidazo[1,2-a]pyrazin-8-amine
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C26H28N8O2
 1
1 IC50 = 44.1 nM
CP0125453
6-(6-aminopyridin-2-yl)-N-[4-[4-(oxetan-3-yl)piperazin-1-yl]phenyl]imidazo[1,2-a]pyrazin-8-amine
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C24H26N8O
 1
1 IC50 = 44.3 nM
CP0238206
5,5-dimethyl-8-[[4-(propylamino)furo[3,2-d]pyrimidin-2-yl]amino]-1H-4,1-benzoxazepin-2-one
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C20H23N5O3
 1
1 IC50 = 45 nM
CP0116125
(4R)-4-[(1R)-1-[[6-(1-methylpyrazol-4-yl)-2,1-benzothiazol-4-yl]oxy]ethyl]pyrrolidin-2-one
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C17H18N4O2S
 1
1 IC50 = 46 nM
CP0137988
CHEMBL2348857
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C19H17FN6O2
 2
1 IC50 = 47 nM
2 IC50 = 1430 nM
CP0122055
2-N-(3-methyl-2H-indazol-6-yl)-4-N-(2,2,2-trifluoroethyl)furo[3,2-d]pyrimidine-2,4-diamine
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C16H13F3N6O
 1
1 IC50 = 47 nM
CP0169424
3-[8-(3,4-dimethoxyanilino)imidazo[1,2-a]pyrazin-6-yl]-N-methylbenzamide
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C22H21N5O3
 1
1 IC50 = 50.2 nM
CP0125452
6-(3-aminophenyl)-N-[4-[4-(oxetan-3-yl)piperazin-1-yl]phenyl]imidazo[1,2-a]pyrazin-8-amine
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C25H27N7O
 1
1 IC50 = 54.6 nM
CP0265842
(4R)-4-[(1R)-1-[[6-[1-(difluoromethyl)pyrazol-4-yl]-2,1-benzothiazol-4-yl]oxy]ethyl]pyrrolidin-2-one
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C17H16F2N4O2S
 1
1 IC50 = 57 nM
CP0697634
N-(5-aminotetrahydro-2H-pyran-3-yl)-2-(6-fluoro-1-methyl-1H-indazol-3-yl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxamide
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C20H20FN7O2
 2
1 IC50 = 61 nM
2 IC50 = 643 nM
CP0081507
2-N-(3-chloro-4-morpholin-4-ylphenyl)-4-N-(2,2,2-trifluoroethyl)furo[3,2-d]pyrimidine-2,4-diamine
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C18H17ClF3N5O2
 2
1 IC50 = 61 nM
2 IC50 = 69 nM
CP0695454
N-(4-(6-oxa-3-azabicyclo[3.1.1]heptan-3-yl)phenyl)-6-(1H-indazol-6-yl)imidazo[1,2-a]pyrazin-8-amine
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C24H21N7O
 1
1 IC50 = 61.6 nM
CP0314384
7-[[4-(2,2,2-trifluoroethylamino)furo[3,2-d]pyrimidin-2-yl]amino]-3,4-dihydro-1H-quinolin-2-one
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C17H14F3N5O2
 1
1 IC50 = 63 nM
CP0137168
2-(6-fluoro-1-methylindazol-3-yl)-N-(4-methylpiperidin-4-yl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxamide
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C21H22FN7O
 1
1 IC50 = 64 nM
CP0562818
5,5-dimethyl-8-[[4-(2-methylpropylamino)furo[3,2-d]pyrimidin-2-yl]amino]-1H-4,1-benzoxazepin-2-one
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C21H25N5O3
 1
1 IC50 = 64 nM
CP0090804
4-[8-(3,4-dimethoxyanilino)imidazo[1,2-a]pyrazin-6-yl]-2-methylbenzamide
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C22H21N5O3
 1
1 IC50 = 64.1 nM
CP0558837
5-[8-(3,4-dimethoxyanilino)imidazo[1,2-a]pyrazin-6-yl]-2-fluorobenzamide
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C21H18FN5O3
 1
1 IC50 = 67.3 nM
CP0131615
2-[1-[3-(dimethylamino)propyl]-6-methylindazol-3-yl]-N-(1-hydroxy-2-methylpropan-2-yl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxamide
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C24H31N7O2
 2
1 IC50 = 68 nM
2 IC50 = 191 nM
CP0419284
N-[(3R,5S)-5-aminooxan-3-yl]-2-(6-fluoro-1-methylindazol-3-yl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxamide
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C20H20FN7O2
 2
1 IC50 = 68 nM
2 IC50 = 1160 nM
CP0081509
2-N-(1H-indazol-6-yl)-4-N-(2,2,2-trifluoroethyl)furo[3,2-d]pyrimidine-2,4-diamine
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C15H11F3N6O
 2
1 IC50 = 81 nM
2 IC50 = 97 nM
CP0776455
4-(1H-indol-7-ylamino)-2-((1R,2S)-2-aminocyclohexylamino)pyrimidine-5-carboxamide
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C19H23N7O
 1
1 IC50 = 94 nM
CP0400235
3-[8-(3,4-dimethoxyanilino)imidazo[1,2-a]pyrazin-6-yl]-N,N-dimethylbenzamide
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C23H23N5O3
 1
1 IC50 = 112 nM
CP0558966
4-[8-(3,4-dimethoxyanilino)imidazo[1,2-a]pyrazin-6-yl]-3-methylbenzamide
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C22H21N5O3
 1
1 IC50 = 113 nM
CP0283985
N-propan-2-yl-2-(1,5,5-trimethyl-6,7-dihydro-4H-indazol-3-yl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxamide
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C20H26N6O
 1
1 IC50 = 132 nM
CP0137166
N-[(3R,5R)-5-aminooxan-3-yl]-2-(6-fluoro-1-methylindazol-3-yl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxamide
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C20H20FN7O2
 2
1 IC50 = 135 nM
2 IC50 = 376 nM
CP0084715
5-(1H-indol-7-ylamino)-7-[[(3R)-piperidin-3-yl]amino]-3H-pyrido[4,3-d]pyrimidin-4-one
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C20H21N7O
 1
1 IC50 = 165 nM
CP0796446
2-(1H-indol-7-ylamino)-6-((1R,2S)-2-aminocyclohexylamino)nicotinamide
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C20H24N6O
 1
1 IC50 = 165 nM
CP0122056
2,2-dimethyl-6-[[4-(2,2,2-trifluoroethylamino)furo[3,2-d]pyrimidin-2-yl]amino]-4H-1,4-benzoxazin-3-one
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C18H16F3N5O3
 1
1 IC50 = 179 nM
CP0313084
5-((1R,2S)-2-Aminocyclohexylamino)-7-(3,5-dimethoxyphenylamino)-2-phenylimidazo[1,2-c]pyrimidine-8-carboxamide
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C27H31N7O3
 1
1 IC50 = 380 nM
CP0563192
N-propyl-4-[[4-(2,2,2-trifluoroethylamino)furo[3,2-d]pyrimidin-2-yl]amino]benzamide
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C18H18F3N5O2
 1
1 IC50 = 561 nM
CP0138955
7-(3,5-Dimethoxyphenylamino)-5-(2-methylcyclohexylamino)imidazo[1,2-c]pyrimidine-8-carboxamide
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C22H28N6O3
 1
1 IC50 = 1000 nM
CP0244626
7-[[(1R,2S)-2-aminocyclohexyl]amino]-5-[(1-methylindol-7-yl)amino]-3H-pyrido[4,3-d]pyrimidin-4-one
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C22H25N7O
 1
1 IC50 = 1600 nM
CP0002778
4-[(4-methylpiperazin-1-yl)methyl]-N-[4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]benzamide
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C29H31N7O
 4
1 IC50 = 5000 nM
2 IC50 > 10000 nM
3 Kd > 10000 nM
4 Ki = 5000 nM
CP0661487
3-(2,6-Dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea monophosphate
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C26H34Cl2N7O7P
 1
1 IC50 > 10000 nM
CP0148490
2-(7-(3,4-dimethoxyphenyl)imidazo[1,2-c]pyrimidin-5-ylamino)nicotinamide hydrochloride
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C20H18N6O3
 1
1 Ki = 7.5 nM
Clinical Information about the Protein
Target 1 ( Tyrosine-protein kinase SYK (SYK) )
Target Type Successful Target
Disease 9 Target-related Diseases  9
1 Immune thrombocytopenic purpura [ICD-11: 3B64.13]
2 Rheumatoid arthritis [ICD-11: FA20]
3 Cutaneous lupus erythematosus [ICD-11: EB5Z]
4 B-cell lymphoma [ICD-11: 2A86]
5 Diffuse large B-cell lymphoma [ICD-11: 2A81]
6 Chronic lymphocytic leukaemia [ICD-11: 2A82.0]
7 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
8 Asthma [ICD-11: CA23]
9 Thrombosis [ICD-11: DB61-GB90]
Approved Drug(s) 1 Approved Drug  1
1 Fostamatinib Approved
Immune thrombocytopenic purpura
Clinical Trial Drug(s) 8 Clinical Trial Drugs  8
1 Cevidoplenib Phase 2
Rheumatoid arthritis
2 GS-9876 Phase 2
Cutaneous lupus erythematosus
3 GS-9973 Phase 2
B-cell lymphoma
4 Cerdulatinib Phase 2
B-cell lymphoma
5 TAK-659 Phase 2
Diffuse large B-cell lymphoma
6 GSK2646264 Phase 1
Cutaneous lupus erythematosus
7 PRT-062607 Phase 1
Chronic lymphocytic leukaemia
8 tamatinib Clinical trial
Solid tumour/cancer
Discontinued Drug(s) 1 Discontinued Drug  1
1 R-343 Discontinued in Phase 2
Asthma
Investigative Drug(s) 2 Investigative Drugs  2
1 CG-103065 Investigative
Solid tumour/cancer
2 PRT-060318 Investigative
Thrombosis
Target 2 ( SYK messenger RNA (SYK mRNA) )
Target Type Clinical trial Target
Disease 1 Target-related Disease  1
1 Eczema [ICD-11: EA80-EA89]
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 ASN002 Phase 2
Eczema
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT00846 Tyrosine-protein kinase ZAP-70 Homo sapiens, Human