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Assay Detail

CHEMBL1243978

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

Binding
Inhibition of recombinant EphB4R by radioactive phosphotransfer assay in presence of 10 uM ATP
ChEMBL ↗
210
Total Activities
209
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Ephrin type-B receptor 4 (CHEMBL5147) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

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 210 5.46 7.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1242285 — — 1 7.77
CHEMBL1241676 — — 1 7.75
CHEMBL1241581 — — 1 7.35
CHEMBL1242656 — — 1 7.27
CHEMBL1242568 — — 1 7.19
CHEMBL1242199 — — 1 7.02
CHEMBL1242662 — — 1 7.02
CHEMBL1242295 — — 1 6.98
CHEMBL1241484 — — 1 6.97
CHEMBL1242377 — — 1 6.78
CHEMBL1242202 — — 1 6.78
CHEMBL1242664 — — 1 6.77
CHEMBL1081312 — — 1 6.72
CHEMBL1241578 — — 1 6.66
CHEMBL1242294 — — 1 6.64
CHEMBL1233882 — — 1 6.62
CHEMBL1241483 — — 1 6.61
CHEMBL1242026 — — 1 6.60
CHEMBL1242198 — — 1 6.60
CHEMBL1242750 — — 1 6.59
CHEMBL1241678 — — 1 6.59
CHEMBL1242201 — — 1 6.59
CHEMBL1242574 — — 1 6.54
CHEMBL1230790 — — 1 6.50
CHEMBL1242024 — — 1 6.50
CHEMBL1242287 — — 1 6.49
CHEMBL1242293 — — 1 6.47
CHEMBL1242376 — — 1 6.46
CHEMBL1241770 — — 1 6.45
CHEMBL1242852 — — 1 6.45

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1242285 — IC50 = 17.0 nM 7.77
CHEMBL1241676 — IC50 = 18.0 nM 7.75
CHEMBL1241581 — IC50 = 45.0 nM 7.35
CHEMBL1242656 — IC50 = 54.0 nM 7.27
CHEMBL1242568 — IC50 = 64.0 nM 7.19
CHEMBL1242199 — IC50 = 96.0 nM 7.02
CHEMBL1242662 — IC50 = 95.0 nM 7.02
CHEMBL1242295 — IC50 = 105.0 nM 6.98
CHEMBL1241484 — IC50 = 106.0 nM 6.97
CHEMBL1242377 — IC50 = 166.0 nM 6.78
CHEMBL1242202 — IC50 = 166.0 nM 6.78
CHEMBL1242664 — IC50 = 170.0 nM 6.77
CHEMBL1081312 — IC50 = 190.0 nM 6.72
CHEMBL1241578 — IC50 = 220.0 nM 6.66
CHEMBL1242294 — IC50 = 230.0 nM 6.64
CHEMBL1233882 — IC50 = 240.0 nM 6.62
CHEMBL1241483 — IC50 = 244.0 nM 6.61
CHEMBL1242198 — IC50 = 251.0 nM 6.60
CHEMBL1242026 — IC50 = 249.0 nM 6.60
CHEMBL1242201 — IC50 = 258.0 nM 6.59
CHEMBL1241678 — IC50 = 256.0 nM 6.59
CHEMBL1242750 — IC50 = 254.0 nM 6.59
CHEMBL1242574 — IC50 = 290.0 nM 6.54
CHEMBL1242024 — IC50 = 316.0 nM 6.50
CHEMBL1230790 — IC50 = 316.0 nM 6.50
CHEMBL1242287 — IC50 = 322.0 nM 6.49
CHEMBL1242293 — IC50 = 340.0 nM 6.47
CHEMBL1242376 — IC50 = 347.0 nM 6.46
CHEMBL1241770 — IC50 = 352.0 nM 6.45
CHEMBL1242852 — IC50 = 353.0 nM 6.45
CHEMBL1241491 — IC50 = 380.0 nM 6.42
CHEMBL1240554 — IC50 = 456.0 nM 6.34
CHEMBL1241677 — IC50 = 468.0 nM 6.33
CHEMBL1242657 — IC50 = 492.0 nM 6.31
CHEMBL1241768 — IC50 = 519.0 nM 6.29
CHEMBL1242110 — IC50 = 566.0 nM 6.25
CHEMBL1242749 — IC50 = 611.0 nM 6.21
CHEMBL1241945 — IC50 = 628.0 nM 6.20
CHEMBL1242029 — IC50 = 628.0 nM 6.20
CHEMBL1242755 — IC50 = 660.0 nM 6.18
CHEMBL1241490 — IC50 = 675.0 nM 6.17
CHEMBL1242114 — IC50 = 737.0 nM 6.13
CHEMBL1242660 — IC50 = 760.0 nM 6.12
CHEMBL1241487 — IC50 = 764.0 nM 6.12
CHEMBL1242853 — IC50 = 871.0 nM 6.06
CHEMBL1242748 — IC50 = 882.0 nM 6.05
CHEMBL939 GEFITINIB IC50 = 1000.0 nM 6.00
CHEMBL1242378 — IC50 = 1000.0 nM 6.00
CHEMBL1241579 — IC50 = 1000.0 nM 6.00
CHEMBL1242111 — IC50 = 1020.0 nM 5.99