Ki Summary

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Target

Isoform Truncated 1 of E3 ubiquitin-protein ligase CBL-B [36-427]

Ligand

BDBM585804

Substrate/Competitor

n/a

Meas. Tech.

Cbl-b Displacement Assay (Cbl-b Inhibition Assay low)

IC50

<1±n/a nM

Citation

Sands, AT; Bence, NF; Zapf, CW; Cohen, F; Wang, C; Cummins, T; Tanaka, H; Shunatona, H; Cardozo, M; Weiss, D; Gosling, J Cyano cyclobutyl compounds for CBL-B inhibition and uses thereof US Patent US11530229 Publication Date 12/20/2022

More Info.:

Get all data from this article, Assay Method

Isoform Truncated 1 of E3 ubiquitin-protein ligase CBL-B [36-427]

Name:

Isoform Truncated 1 of E3 ubiquitin-protein ligase CBL-B [36-427]

Synonyms:

CBLB | CBLB_HUMAN | E3 ubiquitin-protein ligase CBL-B [36-427] | RNF56

Type:

Enzyme Catalytic Domain

Mol. Mass.:

45487.32

Organism:

Homo sapiens (Human)

Description:

aa 36-427 (sequence in paper SEQ ID No: 1)

Residue:

392

Sequence:

PKQAAADRRTVEKTWKLMDKVVRLCQNPKLQLKNSPPYILDILPDTYQHLRLILSKYDDN
QKLAQLSENEYFKIYIDSLMKKSKRAIRLFKEGKERMYEEQSQDRRNLTKLSLIFSHMLA
EIKAIFPNGQFQGDNFRITKADAAEFWRKFFGDKTIVPWKVFRQCLHEVHQISSGLEAMA
LKSTIDLTCNDYISVFEFDIFTRLFQPWGSILRNWNFLAVTHPGYMAFLTYDEVKARLQK
YSTKPGSYIFRLSCTRLGQWAIGYVTGDGNILQTIPHNKPLFQALIDGSREGFYLYPDGR
SYNPDLTGLCEPTPHDHIKVTQEQYELYCEMGSTFQLCKICAENDKDVKIEPCGHLMCTS
CLTAWQESDGQGCPFCRCEIKGTEPIIVDPFD

BDBM585804

n/a

Name

BDBM585804

Synonyms:

US11530229, Compound 19

Type

Small organic molecule

Emp. Form.

C31H33F3N6O

Mol. Mass.

562.6285

SMILES

C[C@H]1CCCN(Cc2cc3C(=O)N(Cc3c(c2)C(F)(F)F)c2cccc(c2)[C@@]2(Cc3nncn3C)C[C@@H](C2)C#N)C1 |r,wU:36.42,wD:27.29,1.0,(-10.75,-3.13,;-9.21,-3.13,;-8.44,-4.47,;-6.9,-4.47,;-6.13,-3.13,;-6.9,-1.8,;-6.13,-.47,;-4.59,-.47,;-3.82,.87,;-2.28,.87,;-1.25,2.01,;-1.57,3.52,;.16,1.39,;-0,-.15,;-1.51,-.47,;-2.28,-1.8,;-3.82,-1.8,;-1.51,-3.13,;-2.28,-4.47,;.03,-3.13,;-.74,-4.47,;1.49,2.16,;1.49,3.7,;2.82,4.47,;4.16,3.7,;4.16,2.16,;2.82,1.39,;5.49,1.39,;4.16,.62,;4.16,-.92,;2.91,-1.83,;3.39,-3.29,;4.93,-3.29,;5.4,-1.83,;6.87,-1.35,;6.58,.3,;7.67,1.39,;6.58,2.48,;9.21,1.39,;10.75,1.39,;-8.44,-1.8,)|

Structure