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. 2010 Mar 19;160(1):1–19. doi: 10.1111/j.1476-5381.2010.00661.x

Table 2.

Various chemotypes present in GSK3β inhibitor molecules

Chemotype structure Chemotype name No. of molecules Off-target kinases
Inline graphic Azaindole 733 PKA, Erk2, EGFR, CK1, CDK1, VEGFR, PKCalpha, PKCbeta, PKCgamma, CDK1/Cyclin B, c-Met, TAK1A, c-Kit, Flt3, KDR, Jak3, Syk
Inline graphic Benzimidazole 880 CDK2/Cyclin A, Src, Aur2, Lck, EGFR, VEGFR2, erbB2
Inline graphic Benzoxazole 18 CDK5/p25, CDK2/Cyclin A, CDK9/Cyclin T1
Inline graphic Benzthiazole 460 Src, AKT, CDK2/Cyclin A, CDK5/p25, CDK9/Cyclin T1, ILK1, AUR2
Inline graphic Imidazole 3 751 Aur2, CDK5/p25, CK1, CK2, VEGFR, PKA, EGFR, Erk2, HER2
Inline graphic Indole 2 075 PKCalpha, PKCgamma, PKCbeta, CDK1, CDK5, ILK1, MSK1, MEK1, CK2, Chk1, Chk2, p38, AKT1, PDK1, AurA, AurB, Fak, Tie2, EGFR, VEGFR2, ABL1, Src, JNK
Inline graphic Oxazole 2 861 N/A
Inline graphic Piperidine 2 814 Erk2, Aur2, CDK5/p25, EGFR, VEGFR2, CK1, CK2, PKA, CDK1/Cyclin B, CDK1, Src, Syk, MK-2, PRAK, ROCK1, JNK3
Inline graphic Purine 11 CDK2/Cyclin A, Aur 2
Inline graphic Pyrazine 1 378 CDK5/p25, CDK1/Cyclin B, PIM1, CK1, CK2, PKG, PKA, JNK, MAPKK, cRaf, Erk1, Erk2, Src, Srk, Aur2, Syk, VEGFR2
Inline graphic Pyrazole 4 571 AUR2, Erk2, Src, AKT, CDK2/Cyclin A, Syk, MK-2, PRAK
Inline graphic Pyridine 12 944 Aur2, JNK3, CDK2/Cyclin A, Lck, CDK2, EGFR, CK1, CK2, PKA, Erk2, HER2
Inline graphic Pyrimidine 14 880 Aur2, JNK3, Lck, Src, Erk2
Inline graphic Pyrrole 935 CDK5/p25, Erk2, CDK2/Cyclin A, Lck, CDK1, CDK5, JNK3, c-met, CDK4/Cyclin D1, MEK1, CK1
Inline graphic Quinazoline 1 378 Aur2, CDK2/Cyclin A, Src, AKT, Src, Erk, PRAK, MK-2, Syk, Lck, ROCK2, Chk1, PDK1, PKA, JNK, MAPK, SAPK
Inline graphic Thiazole 4 364 CDK5/p25, JNK3, Erk2, VEGFR, CDK1, PKA, EGFR, SYK, Aur2
Inline graphic Thiophene 3 338 EGFR, VEGFR, PDGFR, HER2, Erk2, CK1, CK2, CDK1/Cyclin B, PKA

GSK3β, glycogen synthase kinase-3 beta.