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Assay Detail

CHEMBL678501

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

Binding
Ability to prevent phosphorylation of human fibroblast growth factor receptor 1
ChEMBL ↗
66
Total Activities
66
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Fibroblast growth factor receptor 1 (CHEMBL3650) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Soluble 2-substituted aminopyrido[2,3-d]pyrimidin-7-yl ureas. Structure-activity relationships against selected tyrosine kinases and exploration of in vitro and in vivo anticancer activity.
Schroeder MC, Hamby JM, Connolly CJ, Grohar PJ, Winters RT, Barvian MR, Moore CW, Boushelle SL, Crean SM, Kraker AJ, Driscoll DL, Vincent PW, Elliott WL, Lu GH, Batley BL, Dahring TK, Major TC, Panek RL, Doherty AM, Showalter HD.
J Med Chem (2001) 44 : 1915 -1926
PubMed 11384237 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 66 6.49 7.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL51028 — — 1 7.54
CHEMBL57207 — — 1 7.47
CHEMBL431942 — — 1 7.46
CHEMBL292146 — — 1 7.46
CHEMBL293132 — — 1 7.37
CHEMBL299763 — — 1 7.32
CHEMBL45827 — — 1 7.32
CHEMBL301483 — — 1 7.31
CHEMBL57347 — — 1 7.29
CHEMBL61257 — — 1 7.28
CHEMBL418284 — — 1 7.22
CHEMBL51485 — — 1 7.21
CHEMBL60979 — — 1 7.20
CHEMBL368189 — — 1 7.17
CHEMBL301641 — — 1 7.17
CHEMBL57451 — — 1 7.17
CHEMBL432708 — — 1 7.14
CHEMBL298679 — — 1 7.13
CHEMBL294438 — — 1 7.12
CHEMBL417961 — — 1 7.12
CHEMBL57022 — — 1 7.11
CHEMBL299026 — — 1 7.09
CHEMBL418111 — — 1 7.08
CHEMBL57947 — — 1 7.00
CHEMBL56983 — — 1 6.96
CHEMBL444829 — — 1 6.96
CHEMBL293322 — — 1 6.96
CHEMBL57585 — — 1 6.92
CHEMBL58652 — — 1 6.92
CHEMBL301273 — — 1 6.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL51028 — IC50 = 29.0 nM 7.54
CHEMBL57207 — IC50 = 34.0 nM 7.47
CHEMBL292146 — IC50 = 35.0 nM 7.46
CHEMBL431942 — IC50 = 35.0 nM 7.46
CHEMBL293132 — IC50 = 43.0 nM 7.37
CHEMBL299763 — IC50 = 48.0 nM 7.32
CHEMBL45827 — IC50 = 48.0 nM 7.32
CHEMBL301483 — IC50 = 49.0 nM 7.31
CHEMBL57347 — IC50 = 51.0 nM 7.29
CHEMBL61257 — IC50 = 53.0 nM 7.28
CHEMBL418284 — IC50 = 60.0 nM 7.22
CHEMBL51485 — IC50 = 62.0 nM 7.21
CHEMBL60979 — IC50 = 63.0 nM 7.20
CHEMBL301641 — IC50 = 67.0 nM 7.17
CHEMBL368189 — IC50 = 68.0 nM 7.17
CHEMBL57451 — IC50 = 67.0 nM 7.17
CHEMBL432708 — IC50 = 72.0 nM 7.14
CHEMBL298679 — IC50 = 74.0 nM 7.13
CHEMBL294438 — IC50 = 75.0 nM 7.12
CHEMBL417961 — IC50 = 75.0 nM 7.12
CHEMBL57022 — IC50 = 77.0 nM 7.11
CHEMBL299026 — IC50 = 82.0 nM 7.09
CHEMBL418111 — IC50 = 84.0 nM 7.08
CHEMBL57947 — IC50 = 100.0 nM 7.00
CHEMBL293322 — IC50 = 110.0 nM 6.96
CHEMBL444829 — IC50 = 110.0 nM 6.96
CHEMBL56983 — IC50 = 110.0 nM 6.96
CHEMBL57585 — IC50 = 120.0 nM 6.92
CHEMBL58652 — IC50 = 120.0 nM 6.92
CHEMBL301273 — IC50 = 130.0 nM 6.89
CHEMBL56184 — IC50 = 130.0 nM 6.89
CHEMBL57366 — IC50 = 140.0 nM 6.85
CHEMBL264280 — IC50 = 140.0 nM 6.85
CHEMBL57803 — IC50 = 190.0 nM 6.72
CHEMBL58684 — IC50 = 210.0 nM 6.68
CHEMBL56942 — IC50 = 230.0 nM 6.64
CHEMBL60690 — IC50 = 260.0 nM 6.58
CHEMBL300171 — IC50 = 290.0 nM 6.54
CHEMBL443262 — IC50 = 300.0 nM 6.52
CHEMBL417208 — IC50 = 320.0 nM 6.50
CHEMBL291777 — IC50 = 340.0 nM 6.47
CHEMBL57323 — IC50 = 400.0 nM 6.40
CHEMBL416501 — IC50 = 420.0 nM 6.38
CHEMBL298620 — IC50 = 450.0 nM 6.35
CHEMBL299687 — IC50 = 600.0 nM 6.22
CHEMBL294711 — IC50 = 610.0 nM 6.21
CHEMBL56236 — IC50 = 710.0 nM 6.15
CHEMBL57761 — IC50 = 1300.0 nM 5.89
CHEMBL57475 — IC50 = 1800.0 nM 5.75
CHEMBL56380 — IC50 = 2000.0 nM 5.70