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Assay Detail

CHEMBL873338

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Functional
Inhibition of human epidermal growth factor receptor (EGFR) autophosphorylation
ChEMBL ↗
83
Total Activities
83
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Epidermal growth factor receptor (CHEMBL203) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Optimization of 6,7-disubstituted-4-(arylamino)quinoline-3-carbonitriles as orally active, irreversible inhibitors of human epidermal growth factor receptor-2 kinase activity.
Tsou HR, Overbeek-Klumpers EG, Hallett WA, Reich MF, Floyd MB, Johnson BD, Michalak RS, Nilakantan R, Discafani C, Golas J, Rabindran SK, Shen R, Shi X, Wang YF, Upeslacis J, Wissner A.
J Med Chem (2005) 48 : 1107 -1131
PubMed 15715478 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 83 6.83 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL179363 — — 1 8.15
CHEMBL359629 — — 1 8.00
CHEMBL360519 — — 1 7.96
CHEMBL178573 — — 1 7.82
CHEMBL175557 — — 1 7.80
CHEMBL361343 — — 1 7.70
CHEMBL175556 — — 1 7.70
CHEMBL176199 — — 1 7.64
CHEMBL179726 — — 1 7.62
CHEMBL359630 — — 1 7.62
CHEMBL368702 — — 1 7.58
CHEMBL179052 — — 1 7.52
CHEMBL360958 — — 1 7.51
CHEMBL362232 — — 1 7.51
CHEMBL175558 — — 1 7.50
CHEMBL178654 HKI-357 1.0 1 7.47
CHEMBL179766 — — 1 7.47
CHEMBL180175 — — 1 7.39
CHEMBL179572 — — 1 7.38
CHEMBL179969 — — 1 7.35
CHEMBL179577 — — 1 7.35
CHEMBL180415 — — 1 7.29
CHEMBL434720 — — 1 7.28
CHEMBL180516 — — 1 7.19
CHEMBL178144 — — 1 7.17
CHEMBL179633 — — 1 7.14
CHEMBL179607 — — 1 7.12
CHEMBL178312 — — 1 7.11
CHEMBL607707 PELITINIB 2.0 1 7.10
CHEMBL179164 — — 1 7.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL179363 — IC50 = 7.0 nM 8.15
CHEMBL359629 — IC50 = 10.0 nM 8.00
CHEMBL360519 — IC50 = 11.0 nM 7.96
CHEMBL178573 — IC50 = 15.0 nM 7.82
CHEMBL175557 — IC50 = 16.0 nM 7.80
CHEMBL361343 — IC50 = 20.0 nM 7.70
CHEMBL175556 — IC50 = 20.0 nM 7.70
CHEMBL176199 — IC50 = 23.0 nM 7.64
CHEMBL179726 — IC50 = 24.0 nM 7.62
CHEMBL359630 — IC50 = 24.0 nM 7.62
CHEMBL368702 — IC50 = 26.0 nM 7.58
CHEMBL179052 — IC50 = 30.0 nM 7.52
CHEMBL360958 — IC50 = 31.0 nM 7.51
CHEMBL362232 — IC50 = 31.0 nM 7.51
CHEMBL175558 — IC50 = 32.0 nM 7.50
CHEMBL178654 HKI-357 IC50 = 34.0 nM 7.47
CHEMBL179766 — IC50 = 34.0 nM 7.47
CHEMBL180175 — IC50 = 41.0 nM 7.39
CHEMBL179572 — IC50 = 42.0 nM 7.38
CHEMBL179969 — IC50 = 45.0 nM 7.35
CHEMBL179577 — IC50 = 45.0 nM 7.35
CHEMBL180415 — IC50 = 51.0 nM 7.29
CHEMBL434720 — IC50 = 53.0 nM 7.28
CHEMBL180516 — IC50 = 64.0 nM 7.19
CHEMBL178144 — IC50 = 68.0 nM 7.17
CHEMBL179633 — IC50 = 72.0 nM 7.14
CHEMBL179607 — IC50 = 75.0 nM 7.12
CHEMBL178312 — IC50 = 78.0 nM 7.11
CHEMBL607707 PELITINIB IC50 = 80.0 nM 7.10
CHEMBL179164 — IC50 = 82.0 nM 7.09
CHEMBL180022 NERATINIB IC50 = 92.0 nM 7.04
CHEMBL369088 — IC50 = 98.0 nM 7.01
CHEMBL360662 — IC50 = 100.0 nM 7.00
CHEMBL179652 — IC50 = 100.0 nM 7.00
CHEMBL179659 — IC50 = 111.0 nM 6.96
CHEMBL360028 — IC50 = 110.0 nM 6.96
CHEMBL367492 — IC50 = 125.0 nM 6.90
CHEMBL180227 — IC50 = 130.0 nM 6.89
CHEMBL178290 — IC50 = 140.0 nM 6.85
CHEMBL178958 — IC50 = 151.0 nM 6.82
CHEMBL360780 — IC50 = 163.0 nM 6.79
CHEMBL178199 — IC50 = 165.0 nM 6.78
CHEMBL424959 — IC50 = 185.0 nM 6.73
CHEMBL175513 — IC50 = 188.0 nM 6.73
CHEMBL179527 — IC50 = 195.0 nM 6.71
CHEMBL178096 — IC50 = 210.0 nM 6.68
CHEMBL360979 — IC50 = 214.0 nM 6.67
CHEMBL362611 — IC50 = 221.0 nM 6.66
CHEMBL175492 — IC50 = 223.0 nM 6.65
CHEMBL175621 — IC50 = 238.0 nM 6.62