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Compound Detail

CHEMBL3701238

FUTIBATINIB
💊 Approved Drug
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💊 Approved Drug
C=CC(=O)N1CC[C@H](n2nc(C#Cc3cc(OC)cc(OC)c3)c3c(N)ncnc32)C1
ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID CHEMBL3701238
Name FUTIBATINIB
Phase Approved
Structure Type MOL
InChI Key KEIPNCCJPRMIAX-HNNXBMFYSA-N
Therapeutic ✓ Yes

Known Names

Fgfr-in-1 Futibatinib Lytgobi Tas 120 Tas-120
12
Targets
53
Activities
1
Assay Types
1
PK Parameters
20
Publications
5
Known Names
8
Indications
1
Mechanisms

Molecular Properties

418.5
MW (Da)
1.78
ALogP
8
HBA
1
HBD
108.4
PSA (Ų)
0.51
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
First Approval 2022
Availability Prescription
Chirality Single Enantiomer

Routes of Administration

Oral
USAN Stem -tinib
USAN Year 2019

Extended Properties

Molecular Formula C22H22N6O3
MW 418.46
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -0.80

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
Fibroblast growth factor receptor inhibitor INHIBITOR Fibroblast growth factor receptor ✓ ✓

Indications

Cholangiocarcinoma Neoplasms Neoplasms Biliary Tract Neoplasms Sarcoma Carcinoma, Hepatocellular Urinary Bladder Neoplasms Carcinoma, Non-Small-Cell Lung

ATC Classification

L01EN04
futibatinib
Level 1: ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
Level 2: ANTINEOPLASTIC AGENTS

Activity Summary

IC50 53 meas. best 9.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Fibroblast growth factor receptor 3
CHEMBL2742
 IC50 9.3 9.0114 0.5 7
Fibroblast growth factor receptor 2
CHEMBL4142
 IC50 9.0 8.6383 1.0 12
CC-LP-1
CHEMBL6066762
 IC50 8.89 8.245 1.3 4
Unchecked
CHEMBL612545
 IC50 8.89 8.0825 1.3 4
Fibroblast growth factor receptor 1
CHEMBL3650
 IC50 8.74 8.5014 1.8 7
Fibroblast growth factor receptor 4
CHEMBL3973
 IC50 8.47 8.27 3.4 7
SNU-16
CHEMBL613529
 IC50 8.43 8.3867 3.7 3
RT-112
CHEMBL614145
 IC50 8.17 7.31 6.7 5
NCI-H1581
CHEMBL1075516
 IC50 8.15 8.15 7.0 1
Tyrosine-protein kinase BTK
CHEMBL5251
 IC50 7.02 7.02 94.9 1
SK-HEP1
CHEMBL614912
 IC50 6.82 6.82 152.0 1
Vascular endothelial growth factor receptor 2
CHEMBL279
 IC50 5.63 5.63 2358.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 10001.19 ng.hr.mL-1 Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Fibroblast growth factor receptor 3 IC50 = 0.5 nM 9.3 Inhibition Assay: Purified recombinant human FGFR3 protein was purchased from Ca... -
Fibroblast growth factor receptor 3 IC50 = 0.5 nM 9.3 Measurement of Inhibitory Effect on FGFR3 Kinase Activity: The inhibitory effect... -
Fibroblast growth factor receptor 3 IC50 = 0.53 nM 9.28 Inhibition of human FGFR3 (450 to 758 residues) expressed in Escherichia coli BL... 34129329
Fibroblast growth factor receptor 2 IC50 = 1.0 nM 9.0 Inhibition of human recombinant cytoplasmic domain FGFR2 (8 to 134 residues) inc... 37077386
Fibroblast growth factor receptor 2 IC50 = 1.1 nM 8.96 Inhibition Assay: When setting conditions for the measurement of the inhibitory ... -
Fibroblast growth factor receptor 2 IC50 = 1.1 nM 8.96 FGFR2 Kinase Activity: When setting conditions for the measurement of the inhibi... -
Fibroblast growth factor receptor 2 IC50 = 1.1 nM 8.96 Measurement of Inhibitory Effect on FGFR2 Kinase Activity: When setting conditio... -
Fibroblast growth factor receptor 2 IC50 = 1.1 nM 8.96 Measurement of Inhibitory Effect on FGFR2 Kinase Activity: When setting conditio... -
CC-LP-1 IC50 = 1.3 nM 8.89 Antiproliferative activity against human CC-LP-1 cells assessed as inhibition of... 38267212
Unchecked IC50 = 1.3 nM 8.89 Inhibition of FGFR (unknown origin) 39137454
Fibroblast growth factor receptor 2 IC50 = 1.3 nM 8.89 Inhibition of FGFR2 (unknown origin) 38908103
Fibroblast growth factor receptor 2 IC50 = 1.3 nM 8.89 Inhibition of human recombinant FGFR2 expressed in Escherichia coli BL21 DE3 ass... 36324498
Fibroblast growth factor receptor 2 IC50 = 1.3 nM 8.89 Inhibition of FGFR2 (unknown origin) 34962782
CC-LP-1 IC50 = 1.4 nM 8.85 Antiproliferative activity against human CC-LP-1 cells expressing FGFR2 N550H mu... 38267212
Fibroblast growth factor receptor 3 IC50 = 1.6 nM 8.8 Inhibition of FGFR3 (unknown origin) 34962782
Fibroblast growth factor receptor 3 IC50 = 1.6 nM 8.8 Inhibition of FGFR3 (unknown origin) 38908103
Fibroblast growth factor receptor 3 IC50 = 1.6 nM 8.8 Inhibition of human recombinant FGFR3 expressed in Escherichia coli BL21 DE3 ass... 36324498
Fibroblast growth factor receptor 3 IC50 = 1.6 nM 8.8 Inhibition of human FGFR3 37077386
Fibroblast growth factor receptor 1 IC50 = 1.8 nM 8.74 Inhibition of human FGFR1 37077386
Unchecked IC50 = 1.8 nM 8.74 Antiproliferative activity against human ICC13-7 cells assessed as inhibition of... 38267212

Literature References

PubMed DOI Target Context # Activities
38267212 10.1021/acs.jmedchem.3c01819 RT-112 5
37077386 10.1021/acsmedchemlett.3c00006 ADMET 5
38267212 10.1021/acs.jmedchem.3c01819 Unchecked 4
38267212 10.1021/acs.jmedchem.3c01819 CC-LP-1 4
37077386 10.1021/acsmedchemlett.3c00006 Fibroblast growth factor receptor 2 3
34129329 10.1021/acs.jmedchem.1c00174 Fibroblast growth factor receptor 1 2
37077386 10.1021/acsmedchemlett.3c00006 SNU-16 2
36324498 10.1039/d2md00139j Fibroblast growth factor receptor 2 2
37077386 10.1021/acsmedchemlett.3c00006 Fibroblast growth factor receptor 1 2
34129329 10.1021/acs.jmedchem.1c00174 Mitogen-activated protein kinase; ERK1/ERK2 2
34129329 10.1021/acs.jmedchem.1c00174 Unchecked 2
37077386 10.1021/acsmedchemlett.3c00006 Fibroblast growth factor receptor 3 2
34129329 10.1021/acs.jmedchem.1c00174 Fibroblast growth factor receptor 2 2
- 10.6019/CHEMBL4651402 SARS-CoV-2 2
34129329 10.1021/acs.jmedchem.1c00174 SNU-16 1
34129329 10.1021/acs.jmedchem.1c00174 Huh-7 1
34129329 10.1021/acs.jmedchem.1c00174 NCI-H460 1
34962782 10.1021/acs.jmedchem.1c01719 Fibroblast growth factor receptor 1 1
34962782 10.1021/acs.jmedchem.1c01719 Fibroblast growth factor receptor 2 1
34129329 10.1021/acs.jmedchem.1c00174 NCI-H1581 1

Data from ChEMBL 36 via Core Engine