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ABL proto-oncogene 1, non-receptor tyrosine kinase

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Target id: 1923

Nomenclature: ABL proto-oncogene 1, non-receptor tyrosine kinase

Abbreviated Name: Abl

Family: Abl family

Contents:

Gene and Protein Information Click here for help
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human - 1130 9q34.12 ABL1 ABL proto-oncogene 1, non-receptor tyrosine kinase
Mouse - 1123 2 B Abl1 c-abl oncogene 1, non-receptor tyrosine kinase
Rat - 1143 3p12 Abl1 ABL proto-oncogene 1, non-receptor tyrosine kinase
Previous and Unofficial Names Click here for help
Ab | Abelson murine leukemia viral (v-abl) oncogene homolog 1 | JTK7 | tyrosine-protein kinase ABL1 | ABL proto-oncogene 1
Database Links Click here for help
Alphafold P00519 (Hs), P00520 (Mm)
BRENDA 2.7.10.2
CATH/Gene3D 3.30.505.10
ChEMBL Target CHEMBL1862 (Hs), CHEMBL3099 (Mm)
DrugBank Target P00519 (Hs)
Ensembl Gene ENSG00000097007 (Hs), ENSMUSG00000026842 (Mm), ENSRNOG00000047356 (Rn)
Entrez Gene 25 (Hs), 11350 (Mm), 311860 (Rn)
Human Protein Atlas ENSG00000097007 (Hs)
KEGG Enzyme 2.7.10.2
KEGG Gene hsa:25 (Hs), mmu:11350 (Mm), rno:311860 (Rn)
OMIM 189980 (Hs)
Orphanet ORPHA117691 (Hs)
Pharos P00519 (Hs)
RefSeq Nucleotide NM_005157 (Hs), NM_001112703 (Mm), NM_001100850 (Rn)
RefSeq Protein NP_005148 (Hs), NP_001106174 (Mm), NP_001094320 (Rn)
SynPHARM 80775 (in complex with bafetinib)
78765 (in complex with bosutinib)
78746 (in complex with dasatinib)
78741 (in complex with imatinib)
78747 (in complex with nilotinib)
83605 (in complex with rebastinib)
UniProtKB P00519 (Hs), P00520 (Mm)
Wikipedia ABL1 (Hs)
Selected 3D Structures Click here for help
Image of receptor 3D structure from RCSB PDB
Description:  CRYSTAL STRUCTURE OF THE ABL-SH3 DOMAIN COMPLEXED WITH A DESIGNED HIGH-AFFINITY PEPTIDE LIGAND: IMPLICATIONS FOR SH3-LIGAND INTERACTIONS
PDB Id:  1BBZ
Resolution:  1.65Å
Species:  Human
References:  24
Image of receptor 3D structure from RCSB PDB
Description:  Crystal structure of the c-Abl kinase domain in complex with INNO-406
PDB Id:  2E2B
Ligand:  bafetinib
Resolution:  2.2Å
Species:  Human
References:  14
Image of receptor 3D structure from RCSB PDB
Description:  The crystal structure of human abl1 kinase domain in complex with DCC-2036
PDB Id:  3QRI
Ligand:  rebastinib
Resolution:  2.1Å
Species:  Human
References:  5
Enzyme Reaction Click here for help
EC Number: 2.7.10.2

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Inhibitors
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Ligand Sp. Action Value Parameter Reference
dasatinib Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 10.5 pKd 35
⤷ pKd 10.5 (Kd 3.2x10-11 M) [35]
Description: Binding affinity for the unphosphorylated kinase domain of the human ABL protein.
olverembatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 9.5 pKd 26
⤷ pKd 9.5 (Kd 3.2x10-10 M) [26]
Description: Binding affinity for nonphosphorylated Abl1 as determined using an active-site-dependent competitive binding assay (KINOMEscan).
SIAIS178 Small molecule or natural product Immunopharmacology Ligand Hs Inhibition 9.5 pKd 35
⤷ pKd 9.5 (Kd 3.5x10-10 M) [35]
Description: Binding affinity for the unphosphorylated kinase domain of the human ABL protein.
PD-173955 Small molecule or natural product Primary target of this compound Ligand has a PDB structure Hs Inhibition 9.2 pKd 7
⤷ pKd 9.2 (Kd 5.8x10-10 M) [7]
ZAK inhibitor 6p Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.8 pKd 33
⤷ pKd 7.8 (Kd 1.5x10-8 M) [33]
BO1 Small molecule or natural product Hs Inhibition 7.0 – 7.4 pKi 6,25
⤷ pKi 7.0 – 7.4 (Ki 1x10-7 – 4.4x10-8 M) [6,25]
compound 8h [PMID: 21561767] Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 9.7 pIC50 28
⤷ pIC50 9.7 (IC50 2x10-10 M) [28]
dasatinib Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 9.6 pIC50 17
⤷ pIC50 9.6 (IC50 2.7x10-10 M) [17]
olverembatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 9.5 pIC50 26
⤷ pIC50 9.5 (IC50 3.4x10-10 M) [26]
Description: Inhibition of wild type Abl1 kinase activity was determined using the proprietary FRET-based Z′-Lyte assay.
vamotinib Small molecule or natural product Hs Inhibition 9.3 pIC50 19
⤷ pIC50 9.3 (IC50 4.9x10-10 M) [19]
Description: Inhibition of native ABL kinase activity.
compound 24 [PMID: 23441572] Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Inhibition 9.3 pIC50 8
⤷ pIC50 9.3 (IC50 5x10-10 M) [8]
rebastinib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 9.1 pIC50 5,23
⤷ pIC50 9.1 (IC50 8x10-10 M) [5,23]
bosutinib Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 9.0 pIC50 12
⤷ pIC50 9.0 (IC50 1x10-9 M) [12]
compound 2c [PMID: 24900538] Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.9 pIC50 29
⤷ pIC50 8.9 (IC50 1.2x10-9 M) [29]
flumbatinib Small molecule or natural product Approved drug Click here for species-specific activity table Hs Inhibition 8.9 pIC50 18
⤷ pIC50 8.9 (IC50 1.2x10-9 M) [18]
pexmetinib Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 8.4 pIC50 4
⤷ pIC50 8.4 (IC50 4x10-9 M) [4]
ZAK inhibitor 6p Small molecule or natural product Click here for species-specific activity table Hs Inhibition 8.4 pIC50 33
⤷ pIC50 8.4 (IC50 4x10-9 M) [33]
Description: Inhibition of enzymatic activity determined in a ADP-GloTM assay.
PD-173955 Small molecule or natural product Primary target of this compound Ligand has a PDB structure Hs Inhibition ~8.3 pIC50 20
⤷ pIC50 ~8.3 (IC50 ~5x10-9 M) [20]
ponatinib Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 8.1 pIC50 15
⤷ pIC50 8.1 (IC50 8.6x10-9 M) [15]
bafetinib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 7.6 – 8.2 pIC50 14,16
⤷ pIC50 7.6 – 8.2 (IC50 2.6x10-8 – 5.8x10-9 M) [14,16]
KW-2449 Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.8 pIC50 27
⤷ pIC50 7.8 (IC50 1.4x10-8 M) [27]
nilotinib Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.8 pIC50 21
⤷ pIC50 7.8 (IC50 1.5x10-8 M) [21]
PP121 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.7 pIC50 3
⤷ pIC50 7.7 (IC50 1.8x10-8 M) [3]
compound 33a [PMID: 35944901] Small molecule or natural product Hs Inhibition 7.4 – 7.7 pIC50 22
⤷ pIC50 7.7 (IC50 2.01x10-8 M) [22]
Description: Inhibition of WT BCR-Abl
pIC50 7.4 (IC50 4.37x10-8 M) [22]
Description: Inhibition of BCR-AblT315I
saracatinib Small molecule or natural product Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 7.5 pIC50 13
⤷ pIC50 7.5 (IC50 3x10-8 M) [13]
vodobatinib Small molecule or natural product Hs Inhibition 6.8 – 8.2 pIC50 2
⤷ pIC50 8.2 (IC50 6x10-9 M) [2]
Description: Inhibition of Abl1F311L expressed in in Ba/F3 cells.
pIC50 8.1 (IC50 7x10-9 M) [2]
Description: Inhibition of wild type Abl1 expressed in in Ba/F3 cells.
pIC50 6.8 (IC50 1.65x10-7 M) [2]
Description: Inhibition of Abl1E255V expressed in in Ba/F3 cells.
risvodetinib Small molecule or natural product Click here for species-specific activity table Hs Inhibition 7.3 pIC50 31
⤷ pIC50 7.3 (IC50 4.7x10-8 M) [31]
imatinib Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 6.7 pIC50 14
⤷ pIC50 6.7 (IC50 2.2x10-7 M) [14]
GNF-5 Small molecule or natural product Primary target of this compound Hs Inhibition 6.7 pIC50 34
⤷ pIC50 6.7 (IC50 2.2x10-7 M) [34]
Description: Inhibition of wild-type Abl in vitro.
eCF506 Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Hs Inhibition 6.3 pIC50 10
⤷ pIC50 6.3 (IC50 4.79x10-7 M) [10]
DDR1/2 inhibitor 5n Small molecule or natural product Click here for species-specific activity table Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibition 6.3 pIC50 30
⤷ pIC50 6.3 (IC50 4.94x10-7 M) [30]
Inhibitor Comments
Note that bosutinib has inhibitory activity at other kinases including HCK, LYN and Src.
KW-2449 inhibits Abl1T315I with IC50 of 4nM [27].
Compound 24 [PMID 23441572] inhibits Abl1T315I, Abl1H396P, Abl1Q252H, Abl1M351T and Abl1Y253F with IC50 values between 0.3-0.5nM [8].
Compound 8h [PMID 21561767] inhibits Abl1T315I with IC50 of 0.4nM [28].
Allosteric Modulators
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Ligand Sp. Action Value Parameter Reference
asciminib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Negative 8.6 – 9.5 pIC50 9
⤷ pIC50 8.6 – 9.5 (IC50 2.4x10-9 – 3x10-10 M) [9]
Description: Two assays used: a radiometric filter-binding assay and microfluidic mobility shift technology (Caliper assay).
DiscoveRx KINOMEscan® screen Click here for help
A screen of 72 inhibitors against 456 human kinases. Quantitative data were derived using DiscoveRx KINOMEscan® platform.
http://www.discoverx.com/services/drug-discovery-development-services/kinase-profiling/kinomescan
Reference: 7,32
Key to terms and symbols Click column headers to sort
Target used in screen: ABL1(E255K)-phosphorylated
Ligand Sp. Type Action Value Parameter
bosutinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 10.3 pKd
dasatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 10.3 pKd
PD-173955 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.3 pKd
tozasertib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.5 pKd
vandetanib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.9 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.7 pKd
canertinib Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 7.5 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 7.4 pKd
nilotinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.4 pKd
fedratinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.4 pKd
Target used in screen: ABL1(F317I)-nonphosphorylated
Ligand Sp. Type Action Value Parameter
dasatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 10.0 pKd
bosutinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 9.2 pKd
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 8.7 pKd
PD-173955 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.3 pKd
masitinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.1 pKd
imatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.1 pKd
nilotinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.7 pKd
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.4 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.0 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.3 pKd
Target used in screen: ABL1(F317I)-phosphorylated
Ligand Sp. Type Action Value Parameter
dasatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 10.4 pKd
bosutinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 9.7 pKd
PD-173955 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.3 pKd
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 7.9 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.8 pKd
nilotinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.3 pKd
masitinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.1 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.9 pKd
vandetanib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 6.8 pKd
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 6.6 pKd
Target used in screen: ABL1(F317L)-nonphosphorylated
Ligand Sp. Type Action Value Parameter
dasatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 10.5 pKd
bosutinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 10.0 pKd
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 9.1 pKd
imatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.6 pKd
PD-173955 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.5 pKd
masitinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.0 pKd
nilotinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.9 pKd
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.7 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.3 pKd
vandetanib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.1 pKd
Target used in screen: ABL1(F317L)-phosphorylated
Ligand Sp. Type Action Value Parameter
dasatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 10.7 pKd
bosutinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 10.5 pKd
PD-173955 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.6 pKd
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 7.9 pKd
nilotinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.8 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.7 pKd
vandetanib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.5 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.3 pKd
canertinib Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 7.0 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 7.0 pKd
Target used in screen: ABL1(H396P)-nonphosphorylated
Ligand Sp. Type Action Value Parameter
dasatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 10.6 pKd
bosutinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 10.2 pKd
PD-173955 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.2 pKd
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 8.6 pKd
tozasertib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.5 pKd
nilotinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 8.3 pKd
imatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.2 pKd
vandetanib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 8.0 pKd
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.0 pKd
masitinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.0 pKd
Target used in screen: ABL1(H396P)-phosphorylated
Ligand Sp. Type Action Value Parameter
dasatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 10.3 pKd
bosutinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 10.2 pKd
PD-173955 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.9 pKd
tozasertib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.5 pKd
vandetanib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.8 pKd
nilotinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.7 pKd
axitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.6 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 7.6 pKd
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 7.5 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.4 pKd
Target used in screen: ABL1(M351T)-phosphorylated
Ligand Sp. Type Action Value Parameter
dasatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 10.8 pKd
bosutinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 10.4 pKd
PD-173955 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.3 pKd
tozasertib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.3 pKd
nilotinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.8 pKd
vandetanib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.8 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 7.7 pKd
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 7.5 pKd
axitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.4 pKd
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.4 pKd
Target used in screen: ABL1(Q252H)-nonphosphorylated
Ligand Sp. Type Action Value Parameter
dasatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 10.4 pKd
bosutinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 10.1 pKd
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 9.0 pKd
PD-173955 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.9 pKd
imatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.7 pKd
tozasertib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.4 pKd
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.4 pKd
masitinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.2 pKd
nilotinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 8.0 pKd
vandetanib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.7 pKd
Target used in screen: ABL1(Q252H)-phosphorylated
Ligand Sp. Type Action Value Parameter
bosutinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 10.4 pKd
dasatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 10.2 pKd
PD-173955 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.0 pKd
masitinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.3 pKd
tozasertib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.0 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.0 pKd
vandetanib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.8 pKd
nilotinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.7 pKd
canertinib Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 7.7 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 7.7 pKd
Target used in screen: ABL1(T315I)-nonphosphorylated
Ligand Sp. Type Action Value Parameter
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 8.6 pKd
axitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 8.4 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.1 pKd
tozasertib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.0 pKd
crizotinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.9 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 7.9 pKd
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.7 pKd
bosutinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.7 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.3 pKd
doramapimod Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.2 pKd
Target used in screen: ABL1(T315I)-phosphorylated
Ligand Sp. Type Action Value Parameter
axitinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 8.8 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.5 pKd
bosutinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.4 pKd
NVP-TAE684 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.3 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 8.2 pKd
tozasertib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.0 pKd
crizotinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.0 pKd
vandetanib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.7 pKd
cediranib Small molecule or natural product Hs Inhibitor Inhibition 7.7 pKd
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 7.6 pKd
Target used in screen: ABL1(Y253F)-phosphorylated
Ligand Sp. Type Action Value Parameter
bosutinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 10.4 pKd
dasatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 10.2 pKd
PD-173955 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.1 pKd
tozasertib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.1 pKd
vandetanib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 8.1 pKd
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 8.0 pKd
nilotinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.9 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.6 pKd
masitinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.6 pKd
KW-2449 Small molecule or natural product Hs Inhibitor Inhibition 7.4 pKd
Target used in screen: ABL1-nonphosphorylated
Ligand Sp. Type Action Value Parameter
dasatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 10.5 pKd
bosutinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 9.9 pKd
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 9.2 pKd
imatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 9.0 pKd
PD-173955 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.8 pKd
masitinib Small molecule or natural product Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 8.7 pKd
foretinib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.3 pKd
nilotinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 8.0 pKd
tozasertib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.9 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.4 pKd
Target used in screen: ABL1-phosphorylated
Ligand Sp. Type Action Value Parameter
dasatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 10.3 pKd
bosutinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 10.2 pKd
PD-173955 Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 9.2 pKd
tozasertib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 8.1 pKd
nilotinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.9 pKd
AST-487 Small molecule or natural product Hs Inhibitor Inhibition 7.9 pKd
vandetanib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 7.8 pKd
imatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 7.7 pKd
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.7 pKd
canertinib Small molecule or natural product Immunopharmacology Ligand Hs Inhibitor Inhibition 7.5 pKd
Displaying the top 10 most potent ligands  View all ligands in screen »
EMD Millipore KinaseProfilerTM screen/Reaction Biology Kinase HotspotSM screen Click here for help
A screen profiling 158 kinase inhibitors (Calbiochem Protein Kinase Inhibitor Library I and II, catalogue numbers 539744 and 539745) for their inhibitory activity at 1µM and 10µM against 234 human recombinant kinases using the EMD Millipore KinaseProfilerTM service.

A screen profiling the inhibitory activity of 178 commercially available kinase inhibitors at 0.5µM against a panel of 300 recombinant protein kinases using the Reaction Biology Corporation Kinase HotspotSM platform.

http://www.millipore.com/techpublications/tech1/pf3036
http://www.reactionbiology.com/webapps/main/pages/kinase.aspx

Reference: 1,11
Key to terms and symbols Click column headers to sort
Target used in screen: Abl/ABL1
Ligand Sp. Type Action % Activity remaining at 0.5µM % Activity remaining at 1µM % Activity remaining at 10µM
bosutinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 1.8
dasatinib Small molecule or natural product Approved drug Ligand has a PDB structure Immunopharmacology Ligand Hs Inhibitor Inhibition 2.8
nilotinib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 3.5
Cdk1/2 inhibitor III Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 5.0 -5.0 -5.0
TWS119 Small molecule or natural product Hs Inhibitor Inhibition 5.5 -6.0 -5.0
dorsomorphin Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 7.9 4.0 -4.0
vandetanib Small molecule or natural product Approved drug Ligand has a PDB structure Hs Inhibitor Inhibition 11.7
tozasertib Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 13.8
GSK-3 inhibitor IX Small molecule or natural product Hs Inhibitor Inhibition 19.1 -4.0 6.0
staurosporine Small molecule or natural product Ligand has a PDB structure Hs Inhibitor Inhibition 23.0 19.5 1.5
Displaying the top 10 most potent ligands  View all ligands in screen »
Immunopharmacology Comments
Included in GtoImmuPdb based on its association with leukemia.
Immuno Process Associations
Immuno Process:  Inflammation
Immuno Process:  Antigen presentation
Immuno Process:  Immune regulation
Immuno Process:  Cellular signalling
Immuno Process:  T cell (activation)
Immuno Process:  B cell (activation)
Immuno Process:  Immune system development
Immuno Process:  Cytokine production & signalling
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Chronic myeloid leukemia
Disease Ontology: DOID:8552
OMIM: 608232
Orphanet: ORPHA521
Disease:  Precursor B-cell acute lymphoblastic leukemia
Synonyms: Acute lymphocytic leukemia [Disease Ontology: DOID:9952]
Leukemia, acute lymphoblastic; ALL [OMIM: 613065]
Leukemia, B-cell acute lymphoblastic, susceptibility to [OMIM: 613065]
Disease Ontology: DOID:9952
OMIM: 613065
Orphanet: ORPHA99860
Disease:  Precursor T-cell acute lymphoblastic leukemia
Synonyms: Acute lymphocytic leukemia [Disease Ontology: DOID:9952]
Leukemia, acute lymphoblastic; ALL [OMIM: 613065]
Leukemia, T-cell acute lymphoblastic, susceptibility to [OMIM: 613065]
Disease Ontology: DOID:9952
OMIM: 613065
Orphanet: ORPHA99861

References

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How to cite this page

Abl family: ABL proto-oncogene 1, non-receptor tyrosine kinase. Last modified on 21/02/2023. Accessed on 25/04/2025. IUPHAR/BPS Guide to PHARMACOLOGY, https://www.guidetomalariapharmacology.org/GRAC/ObjectDisplayForward?objectId=1923.