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Target
Mast/stem cell growth factor receptor Kit
Ligand
BDBM610463
Substrate
n/a
Meas. Tech.
ChEMBL_2291593
IC50
>50000±n/a nM
Citation
Hartz, RA; Ahuja, VT; Sivaprakasam, P; Xiao, H; Krause, CM; Clarke, WJ; Kish, K; Lewis, H; Szapiel, N; Ravirala, R; Mutalik, S; Nakmode, D; Shah, D; Burton, CR; Macor, JE; Dubowchik, GM Design, Structure-Activity Relationships, and In Vivo Evaluation of Potent and Brain-Penetrant Imidazo[1,2- J Med Chem 66:4231-4252 (2023) [PubMed]
More Info.:
Target
Name:
Mast/stem cell growth factor receptor Kit
Synonyms:
CD117 antigen | CD_antigen=CD117 | KIT | KIT_HUMAN | Mast/stem cell growth factor receptor Kit (cKIT) | Proto-oncogene c-Kit | Proto-oncogene tyrosine-protein kinase Kit | SCFR | Stem cell growth factor receptor | Tyrosine Kinase c-Kit | Tyrosine-protein kinase Kit | Tyrosine-protein kinase Kit (c-Kit) | c-kit | p-145 c-kit | v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homolog
Type:
Protein
Mol. Mass.:
109869.37
Organism:
Homo sapiens (Human)
Description:
P10721
Residue:
976
Sequence:
MRGARGAWDFLCVLLLLLRVQTGSSQPSVSPGEPSPPSIHPGKSDLIVRVGDEIRLLCTDPGFVKWTFEILDETNENKQNEWITEKAEATNTGKYTCTNKHGLSNSIYVFVRDPAKLFLVDRSLYGKEDNDTLVRCPLTDPEVTNYSLKGCQGKPLPKDLRFIPDPKAGIMIKSVKRAYHRLCLHCSVDQEGKSVLSEKFILKVRPAFKAVPVVSVSKASYLLREGEEFTVTCTIKDVSSSVYSTWKRENSQTKLQEKYNSWHHGDFNYERQATLTISSARVNDSGVFMCYANNTFGSANVTTTLEVVDKGFINIFPMINTTVFVNDGENVDLIVEYEAFPKPEHQQWIYMNRTFTDKWEDYPKSENESNIRYVSELHLTRLKGTEGGTYTFLVSNSDVNAAIAFNVYVNTKPEILTYDRLVNGMLQCVAAGFPEPTIDWYFCPGTEQRCSASVLPVDVQTLNSSGPPFGKLVVQSSIDSSAFKHNGTVECKAYNDVGKTSAYFNFAFKGNNKEQIHPHTLFTPLLIGFVIVAGMMCIIVMILTYKYLQKPMYEVQWKVVEEINGNNYVYIDPTQLPYDHKWEFPRNRLSFGKTLGAGAFGKVVEATAYGLIKSDAAMTVAVKMLKPSAHLTEREALMSELKVLSYLGNHMNIVNLLGACTIGGPTLVITEYCCYGDLLNFLRRKRDSFICSKQEDHAEAALYKNLLHSKESSCSDSTNEYMDMKPGVSYVVPTKADKRRSVRIGSYIERDVTPAIMEDDELALDLEDLLSFSYQVAKGMAFLASKNCIHRDLAARNILLTHGRITKICDFGLARDIKNDSNYVVKGNARLPVKWMAPESIFNCVYTFESDVWSYGIFLWELFSLGSSPYPGMPVDSKFYKMIKEGFRMLSPEHAPAEMYDIMKTCWDADPLKRPTFKQIVQLIEKQISESTNHIYSNLANCSPNRQKPVVDHSVRINSVGSTASSSQPLLVHDDV
Inhibitor
Name:
BDBM610463
Synonyms:
BDBM610464 | BDBM610465 | N-(4-(2-Methylmorpholino)pyridin-3-yl)-2-phenylimidazo[1,2-b]pyridazine-8-carboxamide | US10774086, Example 14
Type:
Small organic molecule
Emp. Form.:
C23H22N6O2
Mol. Mass.:
414.4598
SMILES:
CC1CN(CCO1)c1ccncc1NC(=O)c1ccnn2cc(nc12)-c1ccccc1