Target
Serine/threonine-protein phosphatase 2B catalytic subunit gamma isoform
Ligand
BDBM285698
Substrate
n/a
Meas. Tech.
Calcineurin Phosphatase (CaN) Assay
IC50
377±n/a nM
Citation
 Pettit, SNJones, ADFrydrych, CSThomas, AJGarst, ME Cyclosporins modified on the MeBmt sidechain by heterocyclic rings US Patent  US10077289 Publication Date 9/18/2018 
Target
Name:
Serine/threonine-protein phosphatase 2B catalytic subunit gamma isoform
Synonyms:
CALNA3 | CAM-PRP catalytic subunit | CNA3 | Calcineurin, testis-specific catalytic subunit | Calmodulin-dependent calcineurin A subunit gamma isoform | PP2BC_HUMAN | PPP3CC
Type:
Enzyme Catalytic Domain
Mol. Mass.:
58133.25
Organism:
Homo sapiens (Human)
Description:
n/a
Residue:
512
Sequence:
MSGRRFHLSTTDRVIKAVPFPPTQRLTFKEVFENGKPKVDVLKNHLVKEGRLEEEVALKIINDGAAILRQEKTMIEVDAPITVCGDIHGQFFDLMKLFEVGGSPSNTRYLFLGDYVDRGYFSIECVLYLWSLKINHPKTLFLLRGNHECRHLTDYFTFKQECRIKYSEQVYDACMETFDCLPLAALLNQQFLCVHGGMSPEITSLDDIRKLDRFTEPPAFGPVCDLLWSDPSEDYGNEKTLEHYTHNTVRGCSYFYSYPAVCEFLQNNNLLSIIRAHEAQDAGYRMYRKSQATGFPSLITIFSAPNYLDVYNNKAAVLKYENNVMNIRQFNCSPHPYWLPNFMDVFTWSLPFVGEKVTEMLVNVLNICSDDELISDDEAEGSTTVRKEIIRNKIRAIGKMARVFSILRQESESVLTLKGLTPTGTLPLGVLSGGKQTIETATVEAVEAREAIRGFSLQHKIRSFEEARGLDRINERMPPRKDSIHAGGPMKSVTSAHSHAAHRSDQGKKAHS
  
Inhibitor
Name:
BDBM285698
Synonyms:
US10077289, Compound 6 | [(2S,3R,4R)-3-Hydroxy-5-(1-(3-hydroxypropyl)-1H-imidazol-2-yl)-4-methyl-2-(methylamino) pentanoic acid]1 [(R)-methyl-Sar]3 cyclosporin A
Type:
Small organic molecule
Emp. Form.:
C66H117N13O13
Mol. Mass.:
1300.7145
SMILES:
CC[C@H]1NC(=O)[C@@H]([C@H](O)[C@H](C)Cc2nccn2CCCO)N(C)C(=O)[C@@H](C(C)C)N(C)C(=O)[C@@H](CC(C)C)N(C)C(=O)[C@@H](CC(C)C)N(C)C(=O)[C@H](C)NC(=O)[C@@H](C)NC(=O)[C@@H](CC(C)C)N(C)C(=O)[C@H](NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@@H](C)N(C)C1=O)C(C)C |r|
Structure:
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