Approval Year
| Substance Class |
Protein
Created
by
admin
on
Edited
Tue Apr 01 16:34:18 GMT 2025
by
admin
on
Tue Apr 01 16:34:18 GMT 2025
|
| Protein Type | RECEPTOR |
| Protein Sub Type | GROWTH FACTOR RECEPTOR |
| Sequence Origin | HUMAN |
| Sequence Type | COMPLETE |
| Record UNII |
RO03J093CP
|
| Record Status |
Validated (UNII)
|
| Record Version |
|
-
Download
| Name | Type | Language | ||
|---|---|---|---|---|
|
Preferred Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English |
| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
|
RO03J093CP
Created by
admin on Tue Apr 01 16:34:18 GMT 2025 , Edited by admin on Tue Apr 01 16:34:18 GMT 2025
|
PRIMARY | |||
|
P00533
Created by
admin on Tue Apr 01 16:34:18 GMT 2025 , Edited by admin on Tue Apr 01 16:34:18 GMT 2025
|
PRIMARY |
| From | To |
|---|---|
| 1_7 | 1_34 |
| 1_133 | 1_163 |
| 1_166 | 1_175 |
| 1_170 | 1_183 |
| 1_191 | 1_199 |
| 1_195 | 1_207 |
| 1_208 | 1_216 |
| 1_212 | 1_224 |
| 1_227 | 1_236 |
| 1_240 | 1_267 |
| 1_271 | 1_283 |
| 1_287 | 1_302 |
| 1_305 | 1_309 |
| 1_313 | 1_338 |
| 1_446 | 1_475 |
| 1_482 | 1_491 |
| 1_486 | 1_499 |
| 1_502 | 1_511 |
| 1_515 | 1_531 |
| 1_534 | 1_547 |
| 1_538 | 1_555 |
| 1_558 | 1_567 |
| 1_571 | 1_593 |
| 1_596 | 1_604 |
| 1_600 | 1_612 |
| Glycosylation Link Type | Site |
|---|---|
| N | 1_32 |
| N | 1_49 |
| N | 1_104 |
| N | 1_151 |
| N | 1_172 |
| N | 1_328 |
| N | 1_337 |
| N | 1_389 |
| N | 1_420 |
| N | 1_504 |
| N | 1_544 |
| N | 1_579 |
| N | 1_599 |
| Related Record | Type | Details | ||
|---|---|---|---|---|
|
RADIOLIGAND->TARGET |
|
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|
INHIBITOR -> TARGET |
IC50
|
||
|
INHIBITOR -> TARGET |
BINDING
|
||
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|
INHIBITOR -> TARGET |
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INHIBITOR -> TARGET |
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CONJUGATED TOXIN->TARGET |
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||
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INHIBITOR -> TARGET |
IRREVERSIBLE INHIBITOR
|
||
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INHIBITOR -> TARGET |
IC50
|
||
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INHIBITOR -> TARGET |
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INHIBITOR -> TARGET |
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INHIBITOR -> TARGET |
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INHIBITOR -> TARGET |
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|
PARENT -> CONSTITUENT ALWAYS PRESENT |
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INHIBITOR -> TARGET |
In an in vitro study to test kinase selectivity profile of NRC-2694 (free base) against a panel of 353 kinases, NRC-2694 was found to be effective (0 or 0.1% of DMSO control) against EGFR, EGFR (E746-A750del), EGFR (G719C), EGFR (G719S), EGFR (L747-E749del, A750P), EGFR (L747-S752del, P753S), EGFR (L747-T751del, Sins), EGFR (L858R), EGFR (L861Q), EGFR (S752-I759del), GAK and LOK kinase.
IN-VITRO
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CONJUGATED TOXIN->TARGET | |||
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INHIBITOR -> TARGET |
IRREVERSIBLE INHIBITOR
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INHIBITOR -> TARGET |
BINDING
|
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|
LIGAND->TARGET |
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INHIBITOR -> TARGET | |||
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INHIBITOR -> TARGET |
IC50
|
||
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INHIBITOR -> TARGET |
IC50
|
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INHIBITOR->OFF-TARGET |
IC50
|
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|
LIGAND->TARGET | |||
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CONJUGATED TOXIN->TARGET |
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INHIBITOR -> TARGET | |||
|
INHIBITOR->OFF-TARGET |
IC50
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INHIBITOR -> TARGET |
IC50
|
||
|
INHIBITOR -> TARGET |
IRREVERSIBLE INHIBITOR
|
||
|
INHIBITOR -> TARGET |
|
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|
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INHIBITOR -> TARGET |
IRREVERSIBLE INHIBITOR
|
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|
INHIBITOR -> TARGET |
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INHIBITOR -> TARGET |
|
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INHIBITOR -> TARGET |
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INHIBITOR -> TARGET |
BINDING
|
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|
INHIBITOR -> TARGET |
BINDING
|
||
|
|
INHIBITOR -> TARGET | |||
|
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INHIBITOR -> TARGET |
|
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|
|
WEAK INHIBITOR->TARGET |
IC50
|
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|
INHIBITOR -> TARGET |
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INHIBITOR -> TARGET |
IRREVERSIBLE INHIBITOR
IC50
|
||
|
INHIBITOR -> TARGET |
IC50
|
||
|
INHIBITOR -> TARGET |
IC50
|
||
|
INHIBITOR -> TARGET |
IRREVERSIBLE INHIBITOR
|
||
|
INHIBITOR -> TARGET |
IRREVERSIBLE INHIBITOR
IC50
|
||
|
|
INHIBITOR -> TARGET |
|
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|
CONJUGATED TOXIN->TARGET |
|
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|
|
INHIBITOR -> TARGET |
BINDING
|
||
|
INHIBITOR -> TARGET |
IC50
|
||
|
INHIBITOR -> TARGET |
IC50
|
||
|
|
INHIBITOR -> TARGET |
|
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|
INHIBITOR -> TARGET |
|
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|
INHIBITOR -> TARGET |
|
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|
LIGAND->TARGET | |||
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INHIBITOR -> TARGET | |||
|
INHIBITOR -> TARGET |
IRREVERSIBLE INHIBITOR
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||
|
CONJUGATED TOXIN->TARGET |
|
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|
INHIBITOR -> TARGET | |||
|
INHIBITOR -> TARGET |
IC50
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|
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LIGAND->TARGET |
IMAGING AGENT
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LIGAND->TARGET |
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CONJUGATED TOXIN->TARGET |
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INHIBITOR -> TARGET |
IN-VITRO
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|
INHIBITOR -> TARGET |
IRREVERSIBLE INHIBITOR
IC50
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||
|
INHIBITOR -> TARGET |
IC50
|
||
|
|
INHIBITOR -> TARGET |
IRREVERSIBLE INHIBITOR
|
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|
INHIBITOR -> TARGET |
|
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INHIBITOR -> TARGET |
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INHIBITOR -> TARGET |
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|
INHIBITOR -> TARGET |
Wild type receptor
IRREVERSIBLE INHIBITOR
IC50
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INHIBITOR -> TARGET | |||
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INHIBITOR -> TARGET |
BINDING
|
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INHIBITOR -> TARGET |
BINDING
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|
INHIBITOR -> TARGET | |||
|
RADIOLIGAND->TARGET |
|
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|
INHIBITOR -> TARGET |
irreversible selective inhibitor
IRREVERSIBLE INHIBITOR
IC50
|
||
|
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INHIBITOR -> TARGET |
IRREVERSIBLE INHIBITOR
|
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INHIBITOR -> TARGET | |||
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INHIBITOR -> TARGET | |||
|
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INHIBITOR -> TARGET |
IRREVERSIBLE INHIBITOR
|
||
|
INHIBITOR -> TARGET |
IC50
|
||
|
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INHIBITOR -> TARGET |
Kills egfr expressing cells in tumor micfro
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INHIBITOR -> TARGET |
PRECLINICAL
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INHIBITOR -> TARGET |
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INHIBITOR -> TARGET |
IN-VIVO
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LIGAND->TARGET | |||
|
INHIBITOR -> TARGET |
PRECLINICAL
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|
LIGAND->TARGET |
|
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|
INHIBITOR -> TARGET | |||
|
INHIBITOR -> TARGET |
IN-VITRO
|
Structural Modifications
| Modification Type | Location Site | Location Type | Residue Modified | Extent | Fragment Name | Fragment Approval |
|---|---|---|---|---|---|---|
| AMINO ACID SUBSTITUTION | [1_974] [1_992] [1_1068] [1_1086] [1_1148] [1_1173] | TYROSINE O-PHOSPHATE | 2R86C98KDX | |||
| AMINO ACID SUBSTITUTION | [1_654] | THREONINE PHOSPHATE | 3L4WX7B1EI | |||
| AMINO ACID SUBSTITUTION | [1_1175] | TILARGININE | 27JT06E6GR |
| Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
|---|---|---|---|---|---|---|
| Molecular Formula | CHEMICAL |
|
||||
| MOL_WEIGHT | CHEMICAL |
|