Ki Summary

Reaction Details

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Target

Insulin-like growth factor 1 receptor

Ligand

BDBM50336323

Substrate/Competitor

n/a

Meas. Tech.

ChEMBL_716595 (CHEMBL1670374)

IC50

5±n/a nM

Citation

Jin, M; Kleinberg, A; Cooke, A; Gokhale, PC; Foreman, K; Dong, H; Siu, KW; Bittner, MA; Mulvihill, KM; Yao, Y; Landfair, D; O'Connor, M; Mak, G; Pachter, JA; Wild, R; Rosenfeld-Franklin, M; Ji, Q; Mulvihill, MJ Potent and selective cyclohexyl-derived imidazopyrazine insulin-like growth factor 1 receptor inhibitors with in vivo efficacy. Bioorg Med Chem Lett21:1176-80 (2011) [PubMed] Article

More Info.:

Get all data from this article, Assay Method

Insulin-like growth factor 1 receptor

Name:

Insulin-like growth factor 1 receptor

Synonyms:

Type:

Protein

Mol. Mass.:

154776.79

Organism:

Homo sapiens (Human)

Description:

P08069

Residue:

1367

Sequence:

MKSGSGGGSPTSLWGLLFLSAALSLWPTSGEICGPGIDIRNDYQQLKRLENCTVIEGYLH
ILLISKAEDYRSYRFPKLTVITEYLLLFRVAGLESLGDLFPNLTVIRGWKLFYNYALVIF
EMTNLKDIGLYNLRNITRGAIRIEKNADLCYLSTVDWSLILDAVSNNYIVGNKPPKECGD
LCPGTMEEKPMCEKTTINNEYNYRCWTTNRCQKMCPSTCGKRACTENNECCHPECLGSCS
APDNDTACVACRHYYYAGVCVPACPPNTYRFEGWRCVDRDFCANILSAESSDSEGFVIHD
GECMQECPSGFIRNGSQSMYCIPCEGPCPKVCEEEKKTKTIDSVTSAQMLQGCTIFKGNL
LINIRRGNNIASELENFMGLIEVVTGYVKIRHSHALVSLSFLKNLRLILGEEQLEGNYSF
YVLDNQNLQQLWDWDHRNLTIKAGKMYFAFNPKLCVSEIYRMEEVTGTKGRQSKGDINTR
NNGERASCESDVLHFTSTTTSKNRIIITWHRYRPPDYRDLISFTVYYKEAPFKNVTEYDG
QDACGSNSWNMVDVDLPPNKDVEPGILLHGLKPWTQYAVYVKAVTLTMVENDHIRGAKSE
ILYIRTNASVPSIPLDVLSASNSSSQLIVKWNPPSLPNGNLSYYIVRWQRQPQDGYLYRH
NYCSKDKIPIRKYADGTIDIEEVTENPKTEVCGGEKGPCCACPKTEAEKQAEKEEAEYRK
VFENFLHNSIFVPRPERKRRDVMQVANTTMSSRSRNTTAADTYNITDPEELETEYPFFES
RVDNKERTVISNLRPFTLYRIDIHSCNHEAEKLGCSASNFVFARTMPAEGADDIPGPVTW
EPRPENSIFLKWPEPENPNGLILMYEIKYGSQVEDQRECVSRQEYRKYGGAKLNRLNPGN
YTARIQATSLSGNGSWTDPVFFYVQAKTGYENFIHLIIALPVAVLLIVGGLVIMLYVFHR
KRNNSRLGNGVLYASVNPEYFSAADVYVPDEWEVAREKITMSRELGQGSFGMVYEGVAKG
VVKDEPETRVAIKTVNEAASMRERIEFLNEASVMKEFNCHHVVRLLGVVSQGQPTLVIME
LMTRGDLKSYLRSLRPEMENNPVLAPPSLSKMIQMAGEIADGMAYLNANKFVHRDLAARN
CMVAEDFTVKIGDFGMTRDIYETDYYRKGGKGLLPVRWMSPESLKDGVFTTYSDVWSFGV
VLWEIATLAEQPYQGLSNEQVLRFVMEGGLLDKPDNCPDMLFELMRMCWQYNPKMRPSFL
EIISSIKEEMEPGFREVSFYYSEENKLPEPEELDLEPENMESVPLDPSASSSSLPLPDRH
SGHKAENGPGPGVLVLRASFDERQPYAHMNGGRKNERALPLPQSSTC

BDBM50336323

n/a

Name

BDBM50336323

Synonyms:

CHEMBL1667941 | trans-4-(8-amino-1-(8-fluoro-2-phenylquinolin-7-yl)imidazo[1,5-a]pyrazin-3-yl)-N-(1,3,4-thiadiazol-2-yl)cyclohexanecarboxamide

Type

Small organic molecule

Emp. Form.

C30H25FN8OS

Mol. Mass.

564.636

SMILES

Nc1nccn2c(nc(-c3ccc4ccc(nc4c3F)-c3ccccc3)c12)[C@H]1CC[C@@H](CC1)C(=O)Nc1nncs1 |r,wU:27.31,wD:30.38,(36.37,-27.21,;36.37,-28.75,;35.04,-29.52,;35.04,-31.06,;36.38,-31.83,;37.72,-31.05,;39.19,-31.52,;40.09,-30.27,;39.17,-29.02,;39.94,-27.7,;39.17,-26.37,;39.94,-25.04,;41.49,-25.04,;42.25,-23.71,;43.78,-23.71,;44.55,-25.04,;43.78,-26.37,;42.25,-26.37,;41.48,-27.7,;42.25,-29.04,;46.09,-25.04,;46.85,-26.38,;48.39,-26.38,;49.16,-25.04,;48.39,-23.7,;46.85,-23.71,;37.71,-29.51,;39.67,-32.98,;41.18,-33.28,;41.66,-34.75,;40.63,-35.9,;39.12,-35.58,;38.64,-34.12,;41.11,-37.36,;40.32,-38.69,;42.65,-37.38,;43.4,-38.72,;44.94,-38.9,;45.24,-40.41,;43.9,-41.16,;42.77,-40.12,)|

Structure