LINSITINIB

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Search structure


Synonyms	ASP-7487 Linsitinib OSI-906 OSI-906AA
Status
Molecule Category	Free-form
UNII	15A52GPT8T

Structure


InChI Key	PKCDDUHJAFVJJB-VLZXCDOPSA-N
Smiles	C[C@]1(O)C[C@@H](c2nc(-c3ccc4ccc(-c5ccccc5)nc4c3)c3c(N)nccn32)C1
InChI	InChI=1S/C26H23N5O/c1-26(32)14-19(15-26)25-30-22(23-24(27)28-11-12-31(23)25)18-8-7-17-9-10-20(29-21(17)13-18)16-5-3-2-4-6-16/h2-13,19,32H,14-15H2,1H3,(H2,27,28)/t19-,26+

Physicochemical Descriptors

Property Name	Value
Molecular Formula	C26H23N5O
Molecular Weight	421.5
AlogP	4.82
Hydrogen Bond Acceptor	6.0
Hydrogen Bond Donor	2.0
Number of Rotational Bond	3.0
Polar Surface Area	89.33
Molecular species	NEUTRAL
Aromatic Rings	5.0
Heavy Atoms	32.0

Pharmacology

Mechanism of Action	Action	Reference
Insulin receptor inhibitor	INHIBITOR	PubMed PubMed PubMed

Targets	EC50(nM)	IC50(nM)	Kd(nM)	Ki(nM)	Inhibition(%)
Enzyme Kinase Protein Kinase TK protein kinase group Tyrosine protein kinase InsR family	-	2-126	-	-	-
Transporter Primary active transporter ATP-binding cassette ABCG subfamily	104	-	-	-	-

	EC50(nM)	IC50(nM)	Kd(nM)	Ki(nM)	Inhibition(%)
Homo sapiens	104	2-126	-	-	-
Mus musculus	-	-	-	-	104-164

Target Conservation


Protein: Insulin receptor Description: Insulin receptor Organism : Homo sapiens P06213 ENSG00000171105











Protein: Insulin-like growth factor I receptor Description: Insulin-like growth factor 1 receptor Organism : Homo sapiens P08069 ENSG00000140443

Cross References

Resources	Reference
ChEMBL	CHEMBL1091644
DrugBank	DB06075
FDA SRS	15A52GPT8T
Guide to Pharmacology	7423
SureChEMBL	SCHEMBL400735
ZINC	ZINC000100071817

CONTENTS

EcoDrug+ was developed under the PREMIER Innovative Medicines Initiative 2 Joint Undertaking (JU) under grant agreement No 875508. The JU receives support from the EU’s Horizon 2020 research and innovation programme and the European Federation of Pharmaceutical Industries and Associations (EFPIA). The views reflect only the authors’ perspective and the JU is not responsible for any use that may be made of the information EcoDrug+ contains.

Elements of EcoDrug+ were developed under the Biocenter Finland Drug Discovery and Chemical Biology network. CSC-IT Center for Science Ltd is thanked for providing computational resources. Credit is given to Ensembl for collecting species images (provided under public domain licences such as Wikimedia and NHGRI).

Content of EcoDrug+ is provided without guarantee for correctness.

Cite Us:

Ashenafi Legehar, Siobhán Monaghan, Mael Briand, Akseli Niemelä, Leo Ghemtio, Ziaurrehman Tanoli, A Ross Brown, Charles R Tyler, Henri Xhaard, EcoDrug PLUS: an advanced database for drug target conservation analysis and environmental risk assessment, Nucleic Acids Research, 2025, gkaf1251 Read...

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Last update: Monday, 3 November 2025