ISDA: 12FJ

Deposition Date 2026-04-02

Release Date 2026-08-05

Last Version Date 2026-08-05

Entry Detail

PDB ID:

12FJ

Keywords:

TRANSFERASE

Title:

Crystal structure of 6-fluoropyrazolo[1,5-a]pyridine derivative bound to KIT

Biological Source:

Source Organism(s):

Homo sapiens (Taxon ID: 9606)

Expression System(s):

Spodoptera frugiperda

Method Details:

Experimental Method:

X-RAY DIFFRACTION

Resolution:

2.63 Å

R-Value Free:

0.32

R-Value Work:

0.24

Space Group:

P 21 21 21

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Macromolecular Entities

Structures with similar UniProt ID

Structural Superimposition Protein Blast

Polymer Type:polypeptide(L)
Molecule:Mast/stem cell growth factor
Gene (Uniprot):KIT
Chain IDs:A (auth: AAA)
Chain Length:339
Number of Molecules:1
Biological Source:Homo sapiens

UniProt ID:P10721 Pfam ID:PF07714 EC:2.7.10.1

Ligand Molecules

A1DJF

Primary Citation

Discovery of a Potent, Orally Bioavailable Small-Molecule Inhibitor of Wildtype KIT with Exceptionally High Kinome Selectivity.

Chen, K.Y, Qu, S, Yan, X, Moon, H, Lamani, M, Wang, Z, Mata, G, Zhu, J, Schweickert, P.G, Sivick, K.E, Huang, H.T, Van Abbema, A.M, Zhao, X, Green, D.W, Jin, L, Young, S.W, Walters, M.J, Walker, N.P, Leleti, M.R, Powers, J.P, Jeffrey, J.L.Show

J.Med.Chem. ? ? ? (2026)

PMID: 42503832 DOI: 10.1021/acs.jmedchem.6c00898

Primary Citation of related structures

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