Pim1 + Imidazo pyridazine

Pim1 + Imidazo pyridazine

Pim1 + Imidazo pyridazine: Human Pim-1 in complex with an Imidazo[1,2-b]pyridazine and a high affinity consensus peptide
PDB Code: 2C3I
Recently we identified inhibitors of the i midazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine type as strong inhibitors for PIM-1 (1). One of the most potent compound of these two inhibitor classes was 1-(3-{6-[(cyclopropylmethyl)amino]imidazo[1,2-b] pyridazine-3-yl}phenyl)ethanone ( imidazo[1,2-b]pyridazine 1) which had an IC 50 for PIM-1 of 61 nM and a dissociation constant measured by ITC of 25nM. Pyrazolopyrimidine-type inhibitors were first described as specific inhibitors of the Src-family of tyrosine kinases with several pyrazolo[3,4-d]pyrimidines having low nanomolar affinity for Lck and anti-cancer activity (2). One of these compounds PP1 was later crystallized in complex with the autoinhibited form of Hck, providing further guidance for drug development (3). Subsequently this scaffold yielded specific inhibitors for glycogen synthase kinase-3 (GSK-3) and members of the CDK family (4, 5). Inhibitors based on the variant pyrazolo[1,5-a]pyrimidine scaffold have also been described with specificity for CDK2 (6) and the KDR kinase domain (7). Additionally, CDK2 has been co-crystallized with both imidazo[1,2-a]pyridine and imidazo[1,2-b]pyridazine (8, 9) compounds (10).

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