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Assay Detail

CHEMBL1243975

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of recombinant c-Src T338I mutant by radioactive phosphotransfer assay in presence of 10 uM ATP
ChEMBL ↗
209
Total Activities
209
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545) ↗
Type UNCHECKED

Publication

Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.
Apsel B, Blair JA, Gonzalez B, Nazif TM, Feldman ME, Aizenstein B, Hoffman R, Williams RL, Shokat KM, Knight ZA.
Nat Chem Biol (2008) 4 : 691 -699
PubMed 18849971 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 209 5.04 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1241481 — — 1 7.60
CHEMBL1242662 — — 1 7.26
CHEMBL1242294 — — 1 6.99
CHEMBL535 SUNITINIB 4.0 1 6.96
CHEMBL1242852 — — 1 6.94
CHEMBL1242295 — — 1 6.69
CHEMBL1081312 — — 1 6.66
CHEMBL1242664 — — 1 6.60
CHEMBL1242475 — — 1 6.58
CHEMBL1242386 — — 1 6.41
CHEMBL1241945 — — 1 6.37
CHEMBL1242201 — — 1 6.37
CHEMBL1242853 — — 1 6.36
CHEMBL1242293 — — 1 6.32
CHEMBL1242202 — — 1 6.20
CHEMBL1242656 — — 1 6.20
CHEMBL1242026 — — 1 6.17
CHEMBL1242285 — — 1 6.14
CHEMBL1336 SORAFENIB 4.0 1 6.11
CHEMBL1242377 — — 1 6.06
CHEMBL1242572 — — 1 6.03
CHEMBL1242757 — — 1 6.00
CHEMBL1242574 — — 1 5.92
CHEMBL1241944 — — 1 5.89
CHEMBL1242385 — — 1 5.89
CHEMBL1242758 — — 1 5.89
CHEMBL1241581 — — 1 5.88
CHEMBL1241484 — — 1 5.82
CHEMBL1241676 — — 1 5.82
CHEMBL939 GEFITINIB 4.0 1 5.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1241481 — IC50 = 25.0 nM 7.60
CHEMBL1242662 — IC50 = 55.0 nM 7.26
CHEMBL1242294 — IC50 = 103.0 nM 6.99
CHEMBL535 SUNITINIB IC50 = 110.0 nM 6.96
CHEMBL1242852 — IC50 = 116.0 nM 6.94
CHEMBL1242295 — IC50 = 206.0 nM 6.69
CHEMBL1081312 — IC50 = 220.0 nM 6.66
CHEMBL1242664 — IC50 = 250.0 nM 6.60
CHEMBL1242475 — IC50 = 261.0 nM 6.58
CHEMBL1242386 — IC50 = 393.0 nM 6.41
CHEMBL1241945 — IC50 = 424.0 nM 6.37
CHEMBL1242201 — IC50 = 431.0 nM 6.37
CHEMBL1242853 — IC50 = 440.0 nM 6.36
CHEMBL1242293 — IC50 = 480.0 nM 6.32
CHEMBL1242656 — IC50 = 630.0 nM 6.20
CHEMBL1242202 — IC50 = 633.0 nM 6.20
CHEMBL1242026 — IC50 = 670.0 nM 6.17
CHEMBL1242285 — IC50 = 729.0 nM 6.14
CHEMBL1336 SORAFENIB IC50 = 780.0 nM 6.11
CHEMBL1242377 — IC50 = 865.0 nM 6.06
CHEMBL1242572 — IC50 = 930.0 nM 6.03
CHEMBL1242757 — IC50 = 1000.0 nM 6.00
CHEMBL1242574 — IC50 = 1200.0 nM 5.92
CHEMBL1241944 — IC50 = 1300.0 nM 5.89
CHEMBL1242758 — IC50 = 1300.0 nM 5.89
CHEMBL1242385 — IC50 = 1300.0 nM 5.89
CHEMBL1241581 — IC50 = 1320.0 nM 5.88
CHEMBL939 GEFITINIB IC50 = 1500.0 nM 5.82
CHEMBL1241484 — IC50 = 1500.0 nM 5.82
CHEMBL1241676 — IC50 = 1500.0 nM 5.82
CHEMBL1242109 — IC50 = 1560.0 nM 5.81
CHEMBL1242031 — IC50 = 1600.0 nM 5.80
CHEMBL1242199 — IC50 = 1650.0 nM 5.78
CHEMBL1242376 — IC50 = 1690.0 nM 5.77
CHEMBL1242114 — IC50 = 1770.0 nM 5.75
CHEMBL1242287 — IC50 = 1900.0 nM 5.72
CHEMBL1241578 — IC50 = 1900.0 nM 5.72
CHEMBL1241487 — IC50 = 2030.0 nM 5.69
CHEMBL1242568 — IC50 = 2030.0 nM 5.69
CHEMBL1242028 — IC50 = 2100.0 nM 5.68
CHEMBL1242198 — IC50 = 2100.0 nM 5.68
CHEMBL1242476 — IC50 = 2200.0 nM 5.66
CHEMBL1242573 — IC50 = 2300.0 nM 5.64
CHEMBL1241861 — IC50 = 2400.0 nM 5.62
CHEMBL1242384 — IC50 = 2400.0 nM 5.62
CHEMBL1240553 — IC50 = 2600.0 nM 5.58
CHEMBL1241485 — IC50 = 2900.0 nM 5.54
CHEMBL1241439 — IC50 = 2900.0 nM 5.54
CHEMBL1233881 — IC50 = 3000.0 nM 5.52
CHEMBL1242756 — IC50 = 3000.0 nM 5.52