Binding Site Information of Target

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Target General Information
Drug Binding Sites of Target
References
Target General Information  Top
Target ID T36959 Target Info
Target Name Activin receptor-like kinase-1 (ACVRL1)
Synonyms Serine/threonine-protein kinase receptor R3; SKR3; Activin receptor-like kinase 1; ALK-1; ACVRLK1; ACVRL1
Target Type Clinical trial Target
Gene Name ACVRL1
Biochemical Class Kinase
UniProt ID
ACVL1_HUMAN
Drug Binding Sites of Target  Top
Ligand Name: 4-(6-(4-(Piperazin-1-yl)phenyl)pyrazolo[1,5-a]pyrimidin-3-yl)quinoline Ligand Info
Structure Description Crystal structure of the ACVRL1 (ALK1) kinase domain bound to LDN-193189 PDB:3MY0
Method X-ray diffraction Resolution 2.65 Å Mutation No [1]
PDB Sequence
MQRTVARQVA
203
LVECVGKGRY
213
GEVWRGLWHG
223
ESVAVKIFSS
233
RDEQSWFRET
243

EIYNTVLLRH
253
DNILGFIASD
263
MTSTQLWLIT
277
HYHEHGSLYD
287
FLQRQTLEPH
297

LALRLAVSAA
307
CGLAHLHVEI
317
FGTQGKPAIA
327
HRDFKSRNVL
337
VKSNLQCCIA
347

DLGLAVMHSQ
357
GSDYLDIGNN
367
PRVGTKRYMA
377
PEVLDEQIRT
387
DCFESYKWTD
397

IWAFGLVLWE
407
IARRTIVNGI
417
VEDYRPPFYD
427
VVPNDPSFED
437
MKKVVCVDQQ
447

TPTIPNRLAA
457
DPVLSGLAQM
467
MRECWYPNPS
477
ARLTALRIKK
487
TLQKIS
Residue
Distance (Å)
VAL208
3.702
VAL216
3.556
ALA227
3.269
LYS229
3.378
GLU242
4.920
LEU257
4.007
LEU275
3.953
THR277
3.700
HIS278
3.661
TYR279
3.500
HIS280
3.724
Residue
Distance (Å)
GLU281
3.093
HIS282
4.169
GLY283
3.362
SER284
4.190
ASP287
3.377
ARG291
3.898
ARG334
3.560
ASN335
3.504
LEU337
3.461
ALA347
3.801
ASP348
3.917
References  Top
REF 1 A small molecule targeting ALK1 prevents Notch cooperativity and inhibits functional angiogenesis. Angiogenesis. 2015 Apr;18(2):209-17.

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