eF-site ID 6p69-AB PDB Code 6p69 Chain A, B click to enlarge Title Crystal structure of FGFR1-Y563C (FGFR4 surrogate) covalently bound to compound 11. Classification TRANSFERASE Compound Fibroblast growth factor receptor 1 Source (FGFR1_HUMAN) Sequence A:  EYELPEDPRWELPRDRLVLGKPLGEGAFGQVVLAEAIGLP NRVTKVAVKMLKSDATEKDLSDLISEMEMMKMIGKHKNII NLLGACTQDGPLYVIVECASKGNLREYLQARRPPEEQLSS KDLVSCAYQVARGMEYLASKKCIHRDLAARNVLVTEDNVM KIADFGLARDIHHIDYYKKTTNGRLPVKWMAPEALFDRIY THQSDVWSFGVLLWEIFTLGGSPYPGVPVEELFKLLKEGH RMDKPSNCTNELYMMMRDCWHAVPSQRPTFKQLVEDLDRI VALTSNQE B:  SEYELPEDPRWELPRDRLVLGKPLGEGAFGQVVLAEAIGL PNRVTKVAVKMLKSDATEKDLSDLISEMEMMKMIGKHKNI INLLGACTQDGPLYVIVECASKGNLREYLQARRPPEEQLS SKDLVSCAYQVARGMEYLASKKCIHRDLAARNVLVTEDNV MKIADFGLARDIHHIDYYKKTTNGRLPVKWMAPEALFDRI YTHQSDVWSFGVLLWEIFTLGGSPYPGVPVEELFKLLKEG HRMDKPSNCTNELYMMMRDCWHAVPSQRPTFKQLVEDLDR IVALTS Description Functional site 1) chain A residue 570 type sequence R description binding site for residue SO4 A 801 source : AC1 2) chain A residue 627 type sequence R description binding site for residue SO4 A 801 source : AC1 3) chain A residue 657 type sequence T description binding site for residue SO4 A 801 source : AC1 4) chain A residue 659 type sequence N description binding site for residue SO4 A 801 source : AC1 5) chain A residue 661 type sequence R description binding site for residue SO4 A 801 source : AC1 6) chain A residue 615 type sequence A description binding site for residue EDO A 802 source : AC2 7) chain A residue 746 type sequence T description binding site for residue EDO A 802 source : AC2 8) chain A residue 747 type sequence F description binding site for residue EDO A 802 source : AC2 9) chain A residue 748 type sequence K description binding site for residue EDO A 802 source : AC2 10) chain A residue 684 type sequence W description binding site for residue EDO A 803 source : AC3 11) chain A residue 701 type sequence Y description binding site for residue EDO A 803 source : AC3 12) chain A residue 718 type sequence R description binding site for residue EDO A 803 source : AC3 13) chain A residue 719 type sequence M description binding site for residue EDO A 803 source : AC3 14) chain A residue 737 type sequence W description binding site for residue EDO A 803 source : AC3 15) chain A residue 484 type sequence L description binding site for residue O21 A 804 source : AC4 16) chain A residue 486 type sequence E description binding site for residue O21 A 804 source : AC4 17) chain A residue 487 type sequence G description binding site for residue O21 A 804 source : AC4 18) chain A residue 492 type sequence V description binding site for residue O21 A 804 source : AC4 19) chain A residue 494 type sequence L description binding site for residue O21 A 804 source : AC4 20) chain A residue 512 type sequence A description binding site for residue O21 A 804 source : AC4 21) chain A residue 514 type sequence K description binding site for residue O21 A 804 source : AC4 22) chain A residue 531 type sequence E description binding site for residue O21 A 804 source : AC4 23) chain A residue 559 type sequence V description binding site for residue O21 A 804 source : AC4 24) chain A residue 561 type sequence V description binding site for residue O21 A 804 source : AC4 25) chain A residue 562 type sequence E description binding site for residue O21 A 804 source : AC4 26) chain A residue 563 type sequence C description binding site for residue O21 A 804 source : AC4 27) chain A residue 564 type sequence A description binding site for residue O21 A 804 source : AC4 28) chain A residue 630 type sequence L description binding site for residue O21 A 804 source : AC4 29) chain A residue 640 type sequence A description binding site for residue O21 A 804 source : AC4 30) chain A residue 641 type sequence D description binding site for residue O21 A 804 source : AC4 31) chain B residue 570 type sequence R description binding site for residue SO4 B 801 source : AC5 32) chain B residue 627 type sequence R description binding site for residue SO4 B 801 source : AC5 33) chain B residue 657 type sequence T description binding site for residue SO4 B 801 source : AC5 34) chain B residue 659 type sequence N description binding site for residue SO4 B 801 source : AC5 35) chain B residue 661 type sequence R description binding site for residue SO4 B 801 source : AC5 36) chain B residue 574 type sequence Q description binding site for residue SO4 B 802 source : AC6 37) chain B residue 659 type sequence N description binding site for residue SO4 B 802 source : AC6 38) chain B residue 661 type sequence R description binding site for residue SO4 B 802 source : AC6 39) chain B residue 699 type sequence S description binding site for residue SO4 B 802 source : AC6 40) chain B residue 684 type sequence W description binding site for residue EDO B 803 source : AC7 41) chain B residue 701 type sequence Y description binding site for residue EDO B 803 source : AC7 42) chain B residue 713 type sequence L description binding site for residue EDO B 803 source : AC7 43) chain B residue 718 type sequence R description binding site for residue EDO B 803 source : AC7 44) chain B residue 719 type sequence M description binding site for residue EDO B 803 source : AC7 45) chain B residue 737 type sequence W description binding site for residue EDO B 803 source : AC7 46) chain B residue 484 type sequence L description binding site for Di-peptide O21 B 804 and CYS B 563 source : AC8 47) chain B residue 492 type sequence V description binding site for Di-peptide O21 B 804 and CYS B 563 source : AC8 48) chain B residue 494 type sequence L description binding site for Di-peptide O21 B 804 and CYS B 563 source : AC8 49) chain B residue 510 type sequence K description binding site for Di-peptide O21 B 804 and CYS B 563 source : AC8 50) chain B residue 514 type sequence K description binding site for Di-peptide O21 B 804 and CYS B 563 source : AC8 51) chain B residue 531 type sequence E description binding site for Di-peptide O21 B 804 and CYS B 563 source : AC8 52) chain B residue 535 type sequence M description binding site for Di-peptide O21 B 804 and CYS B 563 source : AC8 53) chain B residue 559 type sequence V description binding site for Di-peptide O21 B 804 and CYS B 563 source : AC8 54) chain B residue 561 type sequence V description binding site for Di-peptide O21 B 804 and CYS B 563 source : AC8 55) chain B residue 562 type sequence E description binding site for Di-peptide O21 B 804 and CYS B 563 source : AC8 56) chain B residue 564 type sequence A description binding site for Di-peptide O21 B 804 and CYS B 563 source : AC8 57) chain B residue 565 type sequence S description binding site for Di-peptide O21 B 804 and CYS B 563 source : AC8 58) chain B residue 630 type sequence L description binding site for Di-peptide O21 B 804 and CYS B 563 source : AC8 59) chain B residue 640 type sequence A description binding site for Di-peptide O21 B 804 and CYS B 563 source : AC8 60) chain B residue 641 type sequence D description binding site for Di-peptide O21 B 804 and CYS B 563 source : AC8 61) chain B residue 642 type sequence F description binding site for Di-peptide O21 B 804 and CYS B 563 source : AC8 62) chain A residue 730 type MOD_RES sequence Y description Phosphotyrosine; by autocatalysis => ECO:0000269|PubMed:19224897, ECO:0000269|PubMed:8622701 source Swiss-Prot : SWS_FT_FI5 63) chain B residue 730 type MOD_RES sequence Y description Phosphotyrosine; by autocatalysis => ECO:0000269|PubMed:19224897, ECO:0000269|PubMed:8622701 source Swiss-Prot : SWS_FT_FI5 64) chain A residue 484 type BINDING sequence L description source Swiss-Prot : SWS_FT_FI2 65) chain B residue 568 type BINDING sequence N description source Swiss-Prot : SWS_FT_FI2 66) chain B residue 627 type BINDING sequence R description source Swiss-Prot : SWS_FT_FI2 67) chain B residue 641 type BINDING sequence D description source Swiss-Prot : SWS_FT_FI2 68) chain A residue 514 type BINDING sequence K description source Swiss-Prot : SWS_FT_FI2 69) chain A residue 562 type BINDING sequence E description source Swiss-Prot : SWS_FT_FI2 70) chain A residue 568 type BINDING sequence N description source Swiss-Prot : SWS_FT_FI2 71) chain A residue 627 type BINDING sequence R description source Swiss-Prot : SWS_FT_FI2 72) chain A residue 641 type BINDING sequence D description source Swiss-Prot : SWS_FT_FI2 73) chain B residue 484 type BINDING sequence L description source Swiss-Prot : SWS_FT_FI2 74) chain B residue 514 type BINDING sequence K description source Swiss-Prot : SWS_FT_FI2 75) chain B residue 562 type BINDING sequence E description source Swiss-Prot : SWS_FT_FI2 76) chain A residue 623 type ACT_SITE sequence D description Proton acceptor => ECO:0000255|PROSITE-ProRule:PRU00159, ECO:0000255|PROSITE-ProRule:PRU10028, ECO:0000269|PubMed:19224897 source Swiss-Prot : SWS_FT_FI1 77) chain B residue 623 type ACT_SITE sequence D description Proton acceptor => ECO:0000255|PROSITE-ProRule:PRU00159, ECO:0000255|PROSITE-ProRule:PRU10028, ECO:0000269|PubMed:19224897 source Swiss-Prot : SWS_FT_FI1 78) chain A residue 463 type MOD_RES sequence Y description Phosphotyrosine; by autocatalysis => ECO:0000269|PubMed:16507368, ECO:0000269|PubMed:19224897, ECO:0000269|PubMed:8622701 source Swiss-Prot : SWS_FT_FI3 79) chain B residue 463 type MOD_RES sequence Y description Phosphotyrosine; by autocatalysis => ECO:0000269|PubMed:16507368, ECO:0000269|PubMed:19224897, ECO:0000269|PubMed:8622701 source Swiss-Prot : SWS_FT_FI3 80) chain A residue 653 type MOD_RES sequence Y description Phosphotyrosine; by autocatalysis => ECO:0000269|PubMed:16507368, ECO:0000269|PubMed:19224897, ECO:0000269|PubMed:19665973, ECO:0000269|PubMed:8622701 source Swiss-Prot : SWS_FT_FI4 81) chain A residue 654 type MOD_RES sequence Y description Phosphotyrosine; by autocatalysis => ECO:0000269|PubMed:16507368, ECO:0000269|PubMed:19224897, ECO:0000269|PubMed:19665973, ECO:0000269|PubMed:8622701 source Swiss-Prot : SWS_FT_FI4 82) chain B residue 653 type MOD_RES sequence Y description Phosphotyrosine; by autocatalysis => ECO:0000269|PubMed:16507368, ECO:0000269|PubMed:19224897, ECO:0000269|PubMed:19665973, ECO:0000269|PubMed:8622701 source Swiss-Prot : SWS_FT_FI4 83) chain B residue 654 type MOD_RES sequence Y description Phosphotyrosine; by autocatalysis => ECO:0000269|PubMed:16507368, ECO:0000269|PubMed:19224897, ECO:0000269|PubMed:19665973, ECO:0000269|PubMed:8622701 source Swiss-Prot : SWS_FT_FI4 84) chain A residue 484-514 type prosite sequence LGEGAFGQVVLAEAIGLPNRVTKVAVK description PROTEIN_KINASE_ATP Protein kinases ATP-binding region signature. LGEGAFGQVVlAeaigldkdkpnrvtk...VAVK source prosite : PS00107 85) chain A residue 619-631 type prosite sequence CIHRDLAARNVLV description PROTEIN_KINASE_TYR Tyrosine protein kinases specific active-site signature. CIHrDLAARNVLV source prosite : PS00109

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