erlotinib
Ligand Summary
A quinazoline derivative and ANTINEOPLASTIC AGENT that functions as a PROTEIN KINASE INHIBITOR for EGFR associated tyrosine kinase. It is used in the treatment of NON-SMALL CELL LUNG CANCER.
UNII: J4T82NDH7E
PubChem: 44263854
PubChem: 176870
Guide to Pharmacology: 4920
ChEMBL: CHEMBL1079742
ChEMBL: CHEMBL553
DrugCentral: 1045
LyCHI: NUXHNF3XHDN6
Target Activities
EGFR
Epidermal growth factor receptor
75 Activities
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1 – 10 of 75
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 9.17 | |||||
IC50 | 9 | |||||
Ki | 10 | J. Med. Chem., (2014) 57:23:10176 | ||||
Ki | 10 | J. Med. Chem., (2014) 57:23:10176 | ||||
Ki | 10 | Bioorg. Med. Chem. Lett., (2016) 26:2:534 | ||||
Ki | 10 | ACS Med. Chem. Lett., (2016) 7:1:100 | ||||
IC50 | 9.7 | J. Med. Chem., (2010) 53:7:2892 | ||||
Ki | 9.52 | J. Med. Chem., (2014) 57:23:10176 | ||||
Kd | 9.46 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 9.46 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
GAK
Cyclin-G-associated kinase
8 Activities
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1 – 8 of 8
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 8.51 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 8.51 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 8.51 | J. Med. Chem., (2015) 58:8:3393 | ||||
Kd | 8.51 | J Med Chem, (2018) 61:14:6178 | ||||
Kd | 8.51 | J Med Chem, (2019) 62:9:4772 | ||||
Kd | 8.51 | J Med Chem, (2019) 62:5:2830 | ||||
Kd | 8.51 | Bioorg Med Chem, (2020) 28:1:115188 | ||||
Kd | 8.51 | |||||
SLCO2B1
Solute carrier organic anion transporter family member 2B1
4 Activities
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1 – 4 of 4
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 6.28 | |||||
Ki | 6.28 | J. Med. Chem., (2012) 55:10:4740 | ||||
IC50 | 6.26 | J. Med. Chem., (2012) 55:10:4740 | ||||
Ki | 6.28 | INHIBITOR | ||||
STK10
Serine/threonine-protein kinase 10
3 Activities
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1 – 3 of 3
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 7.72 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 7.72 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.72 | |||||
SLK
STE20-like serine/threonine-protein kinase
3 Activities
Items per page:
1 – 3 of 3
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 7.58 | Nat. Biotechnol., (2008) 26:1:127 | ||||
Kd | 7.58 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.59 | |||||
MAP3K19
Mitogen-activated protein kinase kinase kinase 19
2 Activities
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1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Kd | 7.6 | Nat. Biotechnol., (2011) 29:11:1046 | ||||
Kd | 7.6 | |||||
ERBB2
Receptor tyrosine-protein kinase erbB-2
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 7.7 | None, None:None:None | ||||
ERBB3
Receptor tyrosine-protein kinase erbB-3
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 8 | J Med Chem, (2017) 60:7:3002 | ||||