Compile Data Set for Download or QSAR
Report error Found 214 Enz. Inhib. hit(s) with all data for entry = 50022593
TargetReceptor-type tyrosine-protein kinase FLT3(Human)
ARIAD Pharmaceuticals, Inc.

Curated by ChEMBL
LigandPNGBDBM50322535(3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-meth...)
Affinity DataIC50: 0.0400nMAssay Description:Inhibition of FLT3-ITD mutant (unknown origin) expressed in mouse BaF3 cells assessed as inhibition of FLT3-driven cell viability incubated for 72 hr...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetReceptor-type tyrosine-protein kinase FLT3(Human)
ARIAD Pharmaceuticals, Inc.

Curated by ChEMBL
LigandPNGBDBM50322535(3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-meth...)
Affinity DataIC50: 0.0400nMAssay Description:Inhibition of FLT3-ITD F691I mutant (unknown origin) expressed in mouse BaF3 cells assessed as inhibition of FLT3-driven cell viability incubated for...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetALK tyrosine kinase receptor(Human)
ARIAD Pharmaceuticals, Inc.

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 0.600nMAssay Description:Inhibition of human ALK using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetALK tyrosine kinase receptor(Human)
ARIAD Pharmaceuticals, Inc.

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 0.600nMAssay Description:Inhibition of human ALK C1156Y mutant using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase Fer(Human)
ARIAD Pharmaceuticals, Inc.

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 1.30nMAssay Description:Inhibition of human FER using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetALK tyrosine kinase receptor(Human)
ARIAD Pharmaceuticals, Inc.

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 1.40nMAssay Description:Inhibition of human ALK F1174L mutant using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
ARIAD Pharmaceuticals, Inc.

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 1.5nMAssay Description:Inhibition of human EGFR L858R mutant using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetALK tyrosine kinase receptor(Human)
ARIAD Pharmaceuticals, Inc.

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 1.5nMAssay Description:Inhibition of ALK phosphorylation in human SU-DHL-1 cells harboring NPM-ALK fusion protein incubated for 1 hrs by immunoblot analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetReceptor-type tyrosine-protein kinase FLT3(Human)
ARIAD Pharmaceuticals, Inc.

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 1.5nMAssay Description:Inhibition of human FLT3 D835Y mutant using EAIYAAPFAKKK as substrate in presence of [gamma33P]-ATP by HotSpot assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetALK tyrosine kinase receptor(Human)
ARIAD Pharmaceuticals, Inc.

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 1.70nMAssay Description:Inhibition of human ALK L1196M mutant using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetProto-oncogene tyrosine-protein kinase ROS(Human)
ARIAD Pharmaceuticals, Inc.

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 1.90nMAssay Description:Inhibition of human ROS1 using KKKSPGEYVNIEFG as substrate in presence of [gamma33P]-ATP by HotSpot assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetALK tyrosine kinase receptor(Human)
ARIAD Pharmaceuticals, Inc.

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 2.10nMAssay Description:Inhibition of ALK phosphorylation in human L-82 cells harboring NPM-ALK fusion protein incubated for 1 hrs by immunoblot analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetReceptor-type tyrosine-protein kinase FLT3(Human)
ARIAD Pharmaceuticals, Inc.

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 2.10nMAssay Description:Inhibition of human FLT3 using EAIYAAPFAKKK as substrate in presence of [gamma33P]-ATP by HotSpot assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetALK tyrosine kinase receptor(Human)
ARIAD Pharmaceuticals, Inc.

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 3.20nMAssay Description:Inhibition of ALK phosphorylation in human KARPAS-299 cells harboring NPM-ALK fusion protein incubated for 1 hrs by immunoblot analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetTyrosine-protein kinase Fes/Fps(Human)
ARIAD Pharmaceuticals, Inc.

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 3.5nMAssay Description:Inhibition of human FES using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetALK tyrosine kinase receptor(Human)
ARIAD Pharmaceuticals, Inc.

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 3.70nMAssay Description:Inhibition of ALK phosphorylation in human NCI-H3122 cells harboring EML4-ALK variant 1 fusion protein incubated for 1 hrs by immunoblot analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetFocal adhesion kinase 1(Human)
ARIAD Pharmaceuticals, Inc.

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 3.90nMAssay Description:Inhibition of human FAK using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetProtein-tyrosine kinase 6(Human)
ARIAD Pharmaceuticals, Inc.

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 4.10nMAssay Description:Inhibition of human PTK6 using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetTestis-specific serine/threonine-protein kinase 1(Human)
ARIAD Pharmaceuticals, Inc.

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 4.40nMAssay Description:Inhibition of human TSSK1 using KKKVSRSGLYRSPSMPENLNRPR as substrate in presence of [gamma33P]-ATP by HotSpot assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetALK tyrosine kinase receptor(Human)
ARIAD Pharmaceuticals, Inc.

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 4.5nMAssay Description:Inhibition of ALK phosphorylation in human NCI-H2228 cells harboring EML4-ALK variant 3a/3b fusion protein incubated for 1 hrs by immunoblot analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
ARIAD Pharmaceuticals, Inc.

Curated by ChEMBL
LigandPNGBDBM5446(Erlotinib | OSI-774 | N-(3-ethynylphenyl)-6,7-bis(...)
Affinity DataIC50: 4.70nMAssay Description:Inhibition of EGFR 746 to 750 deletion mutant (unknown origin) expressed in mouse BaF3 cells assessed as inhibition of FLT3-driven cell viability inc...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetALK tyrosine kinase receptor(Human)
ARIAD Pharmaceuticals, Inc.

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 4.90nMAssay Description:Inhibition of human ALK G1202R mutant using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetSerine/threonine-protein kinase Chk2(Human)
ARIAD Pharmaceuticals, Inc.

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 5.60nMAssay Description:Inhibition of human CHEK2 I157T mutant using KKKVSRSGLYRSPSMPENLNRPR as substrate in presence of [gamma33P]-ATP by HotSpot assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetSerine/threonine-protein kinase Chk2(Human)
ARIAD Pharmaceuticals, Inc.

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 6.5nMAssay Description:Inhibition of human CHEK2 using KKKVSRSGLYRSPSMPENLNRPR as substrate in presence of [gamma33P]-ATP by HotSpot assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetALK tyrosine kinase receptor(Human)
ARIAD Pharmaceuticals, Inc.

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 6.60nMAssay Description:Inhibition of human ALK R1275Q mutant using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetALK tyrosine kinase receptor(Human)
ARIAD Pharmaceuticals, Inc.

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 6.60nMAssay Description:Inhibition of ALK phosphorylation in human DEL cells harboring NPM-ALK fusion protein incubated for 1 hrs by immunoblot analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetPlatelet-derived growth factor receptor alpha/beta(Mouse)
ARIAD Pharmaceuticals, Inc.

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 9nMAssay Description:Inhibition of EML4-ALK G1269A mutant (unknown origin) expressed in mouse BaF3 cells assessed as inhibition of ALK-driven cell growth incubated for 3 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetPlatelet-derived growth factor receptor alpha/beta(Mouse)
ARIAD Pharmaceuticals, Inc.

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 11nMAssay Description:Inhibition of EML4-ALK V1180L mutant (unknown origin) expressed in mouse BaF3 cells assessed as inhibition of ALK-driven cell growth incubated for 3 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetPlatelet-derived growth factor receptor alpha/beta(Mouse)
ARIAD Pharmaceuticals, Inc.

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 11nMAssay Description:Inhibition of EML4-ALK L1152R mutant (unknown origin) expressed in mouse BaF3 cells assessed as inhibition of ALK-driven cell growth incubated for 3 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetALK tyrosine kinase receptor(Human)
ARIAD Pharmaceuticals, Inc.

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 12nMAssay Description:Inhibition of ALK phosphorylation in human SUPM2 cells harboring NPM-ALK fusion protein incubated for 1 hrs by immunoblot analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetEpidermal growth factor receptor(Human)
ARIAD Pharmaceuticals, Inc.

Curated by ChEMBL
LigandPNGBDBM5446(Erlotinib | OSI-774 | N-(3-ethynylphenyl)-6,7-bis(...)
Affinity DataIC50: 13nMAssay Description:Inhibition of EGFR L858R mutant (unknown origin) expressed in mouse BaF3 cells assessed as inhibition of EGFR-driven cell viability incubated for 72 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetRibosomal protein S6 kinase alpha-2(Human)
ARIAD Pharmaceuticals, Inc.

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 13nMAssay Description:Inhibition of human RPS6kA2 using KKLNRTLSVA as substrate in presence of [gamma33P]-ATP by HotSpot assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetPlatelet-derived growth factor receptor alpha/beta(Mouse)
ARIAD Pharmaceuticals, Inc.

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 14nMAssay Description:Inhibition of EML4-ALK (unknown origin) expressed in mouse BaF3 cells assessed as inhibition of ALK-driven cell viability incubated for 72 hrs by Cel...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetPlatelet-derived growth factor receptor alpha/beta(Mouse)
ARIAD Pharmaceuticals, Inc.

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 14nMAssay Description:Inhibition of native EML4-ALK (unknown origin) expressed in mouse BaF3 cells assessed as inhibition of ALK-driven cell growth incubated for 3 to 5 we...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetLeukocyte tyrosine kinase receptor(Human)
ARIAD Pharmaceuticals, Inc.

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 14nMAssay Description:Inhibition of human LTK using EAIYAAPFAKKK as substrate in presence of [gamma33P]-ATP by HotSpot assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetEchinoderm microtubule-associated protein-like 4(Human)
ARIAD Pharmaceuticals, Inc.

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 14nMAssay Description:Inhibition of EML4-ALK variant 1 (unknown origin) expressed in mouse BaF3 cells assessed as inhibition of EML4-driven cell viability incubated for 72...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetPlatelet-derived growth factor receptor alpha/beta(Mouse)
ARIAD Pharmaceuticals, Inc.

Curated by ChEMBL
LigandPNGBDBM50436850(CHEMBL2403108 | CERITINIB | US10053458, Comparativ...)
Affinity DataIC50: 16nMAssay Description:Inhibition of EML4-ALK V1180L mutant (unknown origin) expressed in mouse BaF3 cells assessed as inhibition of ALK-driven cell growth incubated for 3 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetPlatelet-derived growth factor receptor alpha/beta(Mouse)
ARIAD Pharmaceuticals, Inc.

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 16nMAssay Description:Inhibition of SDC4-ROS1 (unknown origin) expressed in mouse BaF3 cells assessed as inhibition of ROS1-driven cell viability incubated for 72 hrs by C...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetPlatelet-derived growth factor receptor alpha/beta(Mouse)
ARIAD Pharmaceuticals, Inc.

Curated by ChEMBL
LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataIC50: 17nMAssay Description:Inhibition of EML4-ALK L1198F mutant (unknown origin) expressed in mouse BaF3 cells assessed as inhibition of ALK-driven cell growth incubated for 3 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetSyndecan-4(Homo sapiens)
ARIAD Pharmaceuticals, Inc.

Curated by ChEMBL
LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataIC50: 17nMAssay Description:Inhibition of SDC4-ROS1 (unknown origin) expressed in mouse BaF3 cells assessed as inhibition of ROS1-driven cell viability incubated for 72 hrs by C...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetPlatelet-derived growth factor receptor alpha/beta(Mouse)
ARIAD Pharmaceuticals, Inc.

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 18nMAssay Description:Inhibition of CD74-ROS1 (unknown origin) expressed in mouse BaF3 cells assessed as inhibition of ROS1-driven cell viability incubated for 72 hrs by C...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetPlatelet-derived growth factor receptor alpha/beta(Mouse)
ARIAD Pharmaceuticals, Inc.

Curated by ChEMBL
LigandPNGBDBM50362781(CHEMBL1738797 | US9126931, 366 | Alectinib | 12565...)
Affinity DataIC50: 19nMAssay Description:Inhibition of EML4-ALK S1206Y mutant (unknown origin) expressed in mouse BaF3 cells assessed as inhibition of ALK-driven cell growth incubated for 3 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetTyrosine-protein kinase Yes(Human)
ARIAD Pharmaceuticals, Inc.

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 19nMAssay Description:Inhibition of human YES1 using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetPlatelet-derived growth factor receptor alpha/beta(Mouse)
ARIAD Pharmaceuticals, Inc.

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 20nMAssay Description:Inhibition of EML4-ALK L1152P mutant (unknown origin) expressed in mouse BaF3 cells assessed as inhibition of ALK-driven cell growth incubated for 3 ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetReceptor-type tyrosine-protein kinase FLT3(Human)
ARIAD Pharmaceuticals, Inc.

Curated by ChEMBL
LigandPNGBDBM50322535(3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-meth...)
Affinity DataIC50: 21nMAssay Description:Inhibition of FLT3-ITD F691L mutant (unknown origin) expressed in mouse BaF3 cells assessed as inhibition of FLT3-driven cell viability incubated for...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetProto-oncogene tyrosine-protein kinase receptor Ret(Human)
ARIAD Pharmaceuticals, Inc.

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 22nMAssay Description:Inhibition of human RET V804M mutant using RRRRRRRRRRRVYSTDYYRLFNPS as substrate in presence of [gamma33P]-ATP by HotSpot assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetDual specificity protein kinase CLK1(Human)
ARIAD Pharmaceuticals, Inc.

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 23nMAssay Description:Inhibition of human CLK1 using MBP as substrate in presence of [gamma33P]-ATP by HotSpot assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetALK tyrosine kinase receptor(Human)
ARIAD Pharmaceuticals, Inc.

Curated by ChEMBL
LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataIC50: 23nMAssay Description:Inhibition of ALK phosphorylation in human SU-DHL-1 cells harboring NPM-ALK fusion protein incubated for 1 hrs by immunoblot analysisMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetProtein-tyrosine kinase 2-beta(Human)
ARIAD Pharmaceuticals, Inc.

Curated by ChEMBL
LigandPNGBDBM50185140(AP-26113 | Brigatinib | US11248003, Example Brigat...)
Affinity DataIC50: 24nMAssay Description:Inhibition of human PTK2B using poly (Glu, Tyr)4:1 as substrate in presence of [gamma33P]-ATP by HotSpot assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
TargetPlatelet-derived growth factor receptor alpha/beta(Mouse)
ARIAD Pharmaceuticals, Inc.

Curated by ChEMBL
LigandPNGBDBM50306682((R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1...)
Affinity DataIC50: 25nMAssay Description:Inhibition of CD74-ROS1 (unknown origin) expressed in mouse BaF3 cells assessed as inhibition of ROS1-driven cell viability incubated for 72 hrs by C...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/13/2025
Entry Details
PubMed
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